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European Journal of Medicinal Chemistry
Journal Prestige (SJR): 1.266  Citation Impact (citeScore): 5 Number of Followers: 21  Hybrid journal (It can contain Open Access articles)ISSN (Print) 0223-5234 - ISSN (Online) 1768-3254 Published by Elsevier  [2906 journals]
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- Discovery of quinazoline derivatives CZw-124 as a pan-TRK inhibitor with
potent anticancer effects in vitro and in vivo-
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Abstract: Publication date: 5 August 2022Source: European Journal of Medicinal Chemistry, Volume 238Author(s): Tianxiao Wu, Qiaohua Qin, Ruicheng Lv, Nian Liu, Wenbo Yin, Chenzhou Hao, Yin Sun, Chu Zhang, Yixiang Sun, Dongmei Zhao, Maosheng Cheng
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- Tetrahydropyridin-4-ylpicolinoylglycines as novel and orally active prolyl
hydroxylase 2 (PHD2) inhibitors for the treatment of renal anemia-
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Abstract: Publication date: Available online 25 May 2022Source: European Journal of Medicinal ChemistryAuthor(s): Kaijun Su, Zhihong Li, Linjian Zhang, Shaocong Fang, Mingxuan Mao, Zhuoli Sun, Xiaojin Zhang
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- Ring replacement recommender: Ring modifications for improving biological
activity-
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Abstract: Publication date: Available online 23 May 2022Source: European Journal of Medicinal ChemistryAuthor(s): Peter Ertl, Eva Altmann, Sophie Racine, Richard Lewis
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- Design, synthesis, and in vitro protective effect evaluation of
α-carboline derivatives against H2O2-induced cardiomyocyte injury-
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Abstract: Publication date: 5 August 2022Source: European Journal of Medicinal Chemistry, Volume 238Author(s): Rong-Hong Zhang, Dan Yang, Xiang-Ming Liao, Hong Zhang, Guo-Qi Chen, Wen-Li Zhang, Yu-Chan Wang, Cong Wang, Shang-Gao Liao, Meng Zhou, Yong-Lin Wang, Yong-Jun Li
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- Graphical abstract TOC
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Abstract: Publication date: 5 July 2022Source: European Journal of Medicinal Chemistry, Volume 237Author(s):
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- Graphical abstract TOC
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Abstract: Publication date: 5 July 2022Source: European Journal of Medicinal Chemistry, Volume 237Author(s):
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- Graphical abstract TOC Continued
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Abstract: Publication date: 5 July 2022Source: European Journal of Medicinal Chemistry, Volume 237Author(s):
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- Development of sulfonamide-based NLRP3 inhibitors: Further modifications
and optimization through structure-activity relationship studies-
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Abstract: Publication date: Available online 21 May 2022Source: European Journal of Medicinal ChemistryAuthor(s): Yiming Xu, Yulong Xu, Hallie Blevins, Chunqing Guo, Savannah Biby, Xiang-Yang Wang, Changning Wang, Shijun Zhang
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- Ruthenium(II) complexes targeting membrane as biofilm disruptors and
resistance breakers in Staphylococcus aureus bacteria-
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Abstract: Publication date: Available online 21 May 2022Source: European Journal of Medicinal ChemistryAuthor(s): Liqiang Wang, Lianghong Liu, Xuerong Wang, Yanhui Tan, Xuemin Duan, Chunyan Zhang, Jianxin Cheng, Yanshi Xiong, Guijuan Jiang, Jintao Wang, Xiangwen Liao
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- Discovery of precision targeting EZH2 degraders for triple-negative breast
cancer-
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Abstract: Publication date: Available online 20 May 2022Source: European Journal of Medicinal ChemistryAuthor(s): Cheng Wang, Xinye Chen, Xingchen Liu, Dehua Lu, Shang Li, Lailiang Qu, Fucheng Yin, Heng Luo, Yonglei Zhang, Zhongwen Luo, Ningjie Cui, Lingyi Kong, Xiaobing Wang
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- Alzheimer's disease: Updated multi-targets therapeutics are in clinical
and in progress-
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Abstract: Publication date: Available online 20 May 2022Source: European Journal of Medicinal ChemistryAuthor(s): Zhipei Sang, Keren Wang, Jianghong Dong, Lei Tang
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- Small molecules targeting cGAS-STING pathway for autoimmune disease
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Abstract: Publication date: Available online 20 May 2022Source: European Journal of Medicinal ChemistryAuthor(s): Jiannan Zhao, Ruoxuan Xiao, Ruoqing Zeng, Ende He, Ao Zhang
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- Metallofullerenols in biomedical applications
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Abstract: Publication date: Available online 20 May 2022Source: European Journal of Medicinal ChemistryAuthor(s): Jacek Grebowski, Grzegorz Litwinienko
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- Chemical space exploration around indolylarylsulfone scaffold led to a
novel class of highly active HIV-1 NNRTIs with spiro structural features-
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Abstract: Publication date: Available online 20 May 2022Source: European Journal of Medicinal ChemistryAuthor(s): Shenghua Gao, Yusen Cheng, Shu Song, Letian Song, Fabao Zhao, Shujing Xu, Dongwei Kang, Lin Sun, Ping Gao, Erik De Clercq, Christophe Pannecouque, Xinyong Liu, Peng Zhan
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- Structure-based rational design enables efficient discovery of a new
selective and potent AKT PROTAC degrader-
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Abstract: Publication date: Available online 19 May 2022Source: European Journal of Medicinal ChemistryAuthor(s): Cheng-Liang Zhu, Xiaomin Luo, Tian Tian, Zijian Rao, Hanlin Wang, Zhesheng Zhou, Tian Mi, Danni Chen, Yongjin Xu, Yizhe Wu, Jinxin Che, Yubo Zhou, Jia Li, Xiaowu Dong
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- Design, synthesis of DNA-interactive 4-thiazolidinone-based
indolo-/pyrroloazepinone conjugates as potential cytotoxic and
topoisomerase I inhibitors-
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Abstract: Publication date: Available online 18 May 2022Source: European Journal of Medicinal ChemistryAuthor(s): Manasa Kadagathur, Sandip Patra, Geetanjali Devabattula, Joel George, Regur Phanindranath, Arbaz Sujat Shaikh, Dilep Kumar Sigalapalli, Chandraiah Godugu, Narayana Nagesh, Neelima D. Tangellamudi, Nagula Shankaraiah
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- Selective inhibition of histone deacetylase 3 by novel hydrazide based
small molecules as therapeutic intervention for the treatment of cancer-
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Abstract: Publication date: Available online 18 May 2022Source: European Journal of Medicinal ChemistryAuthor(s): Sravani Pulya, Tarun Patel, Milan Paul, Nilanjan Adhikari, Suvankar Banerjee, Ganesh Routholla, Swati Biswas, Tarun Jha, Balaram Ghosh
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- Discovery of novel coumarin-indole derivatives as tubulin polymerization
inhibitors with potent anti-gastric cancer activities-
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Abstract: Publication date: Available online 18 May 2022Source: European Journal of Medicinal ChemistryAuthor(s): Jian Song, Yong-Feng Guan, Wen-Bo Liu, Chun-Hong Song, Xin-Yi Tian, Ting Zhu, Xiang-Jing Fu, Ying-Qiu Qi, Sai-Yang Zhang
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- Discovery of
(2-(pyrrolidin-1-yl)thieno[3,2-d]pyrimidin-4-yl)(3,4,5-trimethoxyphenyl)methanone
as a novel potent tubulin depolymerizing and vascular disrupting agent-
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Abstract: Publication date: Available online 17 May 2022Source: European Journal of Medicinal ChemistryAuthor(s): Chao Tian, Meng Wang, Xueqi Shi, Xuanzhen Chen, Xiaowei Wang, Zhili Zhang, Junyi Liu
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- Design, synthesis of novel triptolide-glucose conjugates targeting glucose
Transporter-1 and their selective antitumor effect-
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Abstract: Publication date: Available online 17 May 2022Source: European Journal of Medicinal ChemistryAuthor(s): Yan Liu, Jiaqing Huang, Min Wu, Bi Liu, Qiaofa Lin, Jingjing Wu, Yuhua Ouyang, Xin Guo, Ruyi Huang, Yongmin Zhang, Jianhua Xu
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- Discovery of 2H-benzo[b][1,4]oxazin-3(4H)-one derivatives as potent and
selective CDK9 inhibitors that enable transient target engagement for the
treatment of hematologic malignancies-
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Abstract: Publication date: Available online 16 May 2022Source: European Journal of Medicinal ChemistryAuthor(s): Xinren Wang, Xiaoyue Liu, Jianhang Huang, Chenhe Liu, Hongmei Li, Cong Wang, Qianqian Hong, Yan Lei, Jiawei Xia, Ziheng Yu, Ruinan Dong, Junyu Xu, Zhenlin Tu, ChunQi Duan, Shuwen Li, Tao Lu, Weifang Tang, Yadong Chen
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- New peptidomimetic rhodesain inhibitors with improved selectivity towards
human cathepsins-
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Abstract: Publication date: Available online 14 May 2022Source: European Journal of Medicinal ChemistryAuthor(s): Sascha Jung, Natalie Fuchs, Christoph Grathwol, Ute A. Hellmich, Annika Wagner, Erika Diehl, Thomas Willmes, Christoph Sotriffer, Tanja Schirmeister
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- Novel deuterated Mnk1/2 protein degrader VNLG-152R analogs: Synthesis, In
vitro Anti-TNBC activities and pharmacokinetics in mice. A strategy for
extending the half-life and patent life of VNLG-152R-
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Abstract: Publication date: Available online 14 May 2022Source: European Journal of Medicinal ChemistryAuthor(s): Puranik Purushottamachar, Elizabeth Thomas, Retheesh S. Thankan, Vincent C.O. Njar
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- Novel flavonoid hybrids as potent antiviral agents against hepatitis A:
Design, synthesis and biological evaluation-
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Abstract: Publication date: Available online 14 May 2022Source: European Journal of Medicinal ChemistryAuthor(s): Shaochun Shi, Xin Zheng, Ryosuke Suzuki, Ziyue Li, Tomoyuki Shiota, Jiayin Wang, Asuka Hirai-Yuki, Qingbo Liu, Masamichi Muramatsu, Shao-Jiang Song
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- Structure-based discovery and development of novel O-GlcNAcase inhibitors
for the treatment of Alzheimer's disease-
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Abstract: Publication date: Available online 13 May 2022Source: European Journal of Medicinal ChemistryAuthor(s): Xiaoli Li, Jinhe Han, Sheshurao Bujaranipalli, Jie He, Eun Young Kim, Hee Kim, Jae Hong Im, Won-Jea Cho
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- Emerging impact of triazoles as anti-tubercular agent
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Abstract: Publication date: Available online 13 May 2022Source: European Journal of Medicinal ChemistryAuthor(s): Anindra Sharma, Anand K. Agrahari, Sanchayita Rajkhowa, Vinod K. Tiwari
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- Glycosylation increases the anti-QS as well as anti-biofilm and
anti-adhesion ability of the cyclo (L-Trp-L-Ser) against Pseudomonas
aeruginosa-
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Abstract: Publication date: Available online 13 May 2022Source: European Journal of Medicinal ChemistryAuthor(s): Yinglu Wang, Lile Pan, Li Li, Ruipin Cao, Qian Zheng, Zuxian Xu, Chang Jer Wu, Hu Zhu
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- From tryptophan to novel mitochondria-disruptive agent, synthesis and
biological evaluation of 1,2,3,6-tetrasubstituted carbazoles-
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Abstract: Publication date: Available online 13 May 2022Source: European Journal of Medicinal ChemistryAuthor(s): Milena Witkowska, Natalia Maciejewska, Małgorzata Ryczkowska, Mateusz Olszewski, Maciej Bagiński, Sławomir Makowiec
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- New TRPM8 blockers exert anticancer activity over castration-resistant
prostate cancer models-
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Abstract: Publication date: Available online 12 May 2022Source: European Journal of Medicinal ChemistryAuthor(s): Veronica Di Sarno, Pia Giovannelli, Alicia Medina-Peris, Tania Ciaglia, Marzia Di Donato, Simona Musella, Gianluigi Lauro, Vincenzo Vestuto, Gerardina Smaldone, Francesca Di Matteo, Giuseppe Bifulco, Gabriella Castoria, Antimo Migliaccio, Asia Fernandez-Carvajal, Pietro Campiglia, Isabel Gomez-Monterrey, Carmine Ostacolo, Alessia Bertamino
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- Study of the anticancer potential of Cd complexes of selenazoyl-hydrazones
and their sulphur isosters-
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Abstract: Publication date: Available online 12 May 2022Source: European Journal of Medicinal ChemistryAuthor(s): Sanja B. Marković, Natalia Maciejewska, Mateusz Olszewski, Aleksandar Višnjevac, Adrián Puerta, José M. Padrón, Irena Novaković, Snežana Kojić, Henrique S. Fernandes, Sérgio F. Sousa, Sandra Ramotowska, Agnieszka Chylewska, Mariusz Makowski, Tamara R. Todorović, Nenad R. Filipović
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- Design and synthesis of proteolysis targeting chimeras (PROTACs) as an
EGFR degrader based on CO-1686-
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Abstract: Publication date: Available online 12 May 2022Source: European Journal of Medicinal ChemistryAuthor(s): Qinlan Li, Qian Guo, Shuyi Wang, Shanhe Wan, Zhonghuang Li, Jiajie Zhang, Xiaoyun Wu
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- Design, synthesis and antitumour activity of novel
5(6)-amino-benzimidazolequinones containing a fused morpholine-
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Abstract: Publication date: Available online 11 May 2022Source: European Journal of Medicinal ChemistryAuthor(s): Haixia Wang, Yao Meng, Jing Yang, Hao Huang, Yifan Zhao, Chuantao Zhu, Cong Wang, Feng-Wu Liu
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- Discovery of a potent, selective and cell active inhibitor of
m6A demethylase ALKBH5-
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Abstract: Publication date: Available online 11 May 2022Source: European Journal of Medicinal ChemistryAuthor(s): Zhen Fang, Bo Mu, Yang Liu, Nihong Guo, Liang Xiong, Yinping Guo, Anjie Xia, Rong Zhang, Hailin Zhang, Rui Yao, Yan Fan, Linli Li, Shengyong Yang, Rong Xiang
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- Design, synthesis and biological evaluation of new parbendazole
derivatives for the treatment of HNSCC-
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Abstract: Publication date: Available online 11 May 2022Source: European Journal of Medicinal ChemistryAuthor(s): Dong Liang, Chen Yu, Zhao Ma, Mingzhao Hu, Jiahui Wang, Xuhui Dong, Lupei Du, Minyong Li
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- Design, synthesis, and biological evaluation of novel pyrazolo
[3,4-d]pyrimidine derivatives as potent PLK4 inhibitors for the treatment
of TRIM37-amplified breast cancer-
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Abstract: Publication date: Available online 10 May 2022Source: European Journal of Medicinal ChemistryAuthor(s): Yin Sun, Yu Sun, Lin Wang, Tianxiao Wu, Wenbo Yin, Jingkai Wang, Yanli Xue, Qiaohua Qin, Yixiang Sun, Huali Yang, Dongmei Zhao, Maosheng Cheng
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- Discovery, enantioselective synthesis of myrtucommulone E analogues as
tyrosyl-DNA phosphodiesterase 2 inhibitors and their biological activities
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Abstract: Publication date: Available online 10 May 2022Source: European Journal of Medicinal ChemistryAuthor(s): Yu Zhang, Hao Yang, Fang-Ting Wang, Xing Peng, Hai-Yang Liu, Qing-Jiang Li, Lin-Kun An
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- Novel 1,3,4-oxadiazole chalcogen analogues: Synthesis and cytotoxic
activity-
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Abstract: Publication date: Available online 10 May 2022Source: European Journal of Medicinal ChemistryAuthor(s): Stefano Zoroddu, Paola Corona, Luca Sanna, Federica Borghi, Valentina Bordoni, Battistina Asproni, Gerard A. Pinna, Luigi Bagella, Gabriele Murineddu
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- Synthesis and Structure–Activity relationships of cyclin-dependent
kinase 11 inhibitors based on a diaminothiazole scaffold-
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Abstract: Publication date: Available online 8 May 2022Source: European Journal of Medicinal ChemistryAuthor(s): Zhengnian Li, Ryosuke Ishida, Yan Liu, Jinhua Wang, Yina Li, Yang Gao, Jie Jiang, Jianwei Che, Jason M. Sheltzer, Matthew B. Robers, Tinghu Zhang, Kenneth D. Westover, Behnam Nabet, Nathanael S. Gray
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- Identification, optimization, and biological evaluation of
3-O-β-chacotriosyl ursolic acid derivatives as novel SARS-CoV-2 entry
inhibitors by targeting the prefusion state of spike protein-
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Abstract: Publication date: Available online 7 May 2022Source: European Journal of Medicinal ChemistryAuthor(s): Hui Li, Chen Cheng, Shanshan Shi, Yan Wu, Yongfeng Gao, Zhihao Liu, Mingjian Liu, Zhaodong Li, Lijian Huo, Xiapyan Pan, Shuwen Liu, Gaopeng Song
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- Design, synthesis, and biological evaluation of trizole-based
heteroaromatic derivatives as Bcr-Abl kinase inhibitors-
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Abstract: Publication date: Available online 6 May 2022Source: European Journal of Medicinal ChemistryAuthor(s): Xiaoyan Pan, Nanxin Liu, Yuying Liu, Qingqing Zhang, Kai Wang, Xueying Liu, Jie Zhang
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- The progress of small-molecules and degraders against BCR-ABL for the
treatment of CML-
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Abstract: Publication date: Available online 6 May 2022Source: European Journal of Medicinal ChemistryAuthor(s): You-lu Pan, Shen-xin Zeng, Rong-rong Hao, Mei-hao Liang, Zheng-rong Shen, Wen-hai Huang
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- Cascade synthetic strategies opening access to medicinal-relevant
aliphatic 3- and 4-membered N-heterocyclic scaffolds-
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Abstract: Publication date: Available online 6 May 2022Source: European Journal of Medicinal ChemistryAuthor(s): Daniel Łowicki, Piotr Przybylski
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- Synthesis of 10,10′-bis(trifluoromethyl) marinopyrrole A derivatives and
evaluation of their antiviral activities in vitro-
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Abstract: Publication date: Available online 6 May 2022Source: European Journal of Medicinal ChemistryAuthor(s): Yaxin Xiao, Jingjing Yang, Liangjing Zou, Pingzhou Wu, Wei Li, Yunzheng Yan, Yuexiang Li, Song Li, Hao Song, Wu Zhong, Yong Qin
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- Identification and development of a series of disubstituted piperazines
for the treatment of Chagas disease-
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Abstract: Publication date: Available online 6 May 2022Source: European Journal of Medicinal ChemistryAuthor(s): Kate McGonagle, Gary J. Tarver, Juan Cantizani, Ignacio Cotillo, Peter G. Dodd, Liam Ferguson, Ian H. Gilbert, Maria Marco, Tim Miles, Claire Naylor, Maria Osuna-Cabello, Christy Paterson, Kevin D. Read, Erika G. Pinto, Jennifer Riley, Paul Scullion, Yoko Shishikura, Frederick Simeons, Laste Stojanovski, Nina Svensen
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- Dual-functional antitumor conjugates improving the anti-metastasis effect
of combretastatin A4 by targeting tubulin polymerization and matrix
metalloproteinases-
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Abstract: Publication date: Available online 5 May 2022Source: European Journal of Medicinal ChemistryAuthor(s): Limin Yang, Xin Ma, Kerong Guo, Jian Li, Chong Zhang, Liqiang Wu
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- Design and synthesis of new quinoline derivatives as selective C-RAF
kinase inhibitors with potent anticancer activity-
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Abstract: Publication date: Available online 5 May 2022Source: European Journal of Medicinal ChemistryAuthor(s): Seyed-Omar Zaraei, Nour N. Al-Ach, Hanan S. Anbar, Randa El-Gamal, Hamadeh Tarazi, Rimas T. Tokatly, Rawan R. Kalla, Mouna A. Munther, Marwa M. Wahba, Aya M. Alshihabi, Mahmoud K. Shehata, Rawan M. Sbenati, Afnan I. Shahin, Raafat El-Awady, Taleb H. Al-Tel, Mohammed I. El-Gamal
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- Discovery of
2-((2-methylbenzyl)thio)-6-oxo-4-(3,4,5-trimethoxyphenyl)-1,6-dihydropyrimidine-5-carbonitrile
as a novel and effective bromodomain and extra-terminal (BET) inhibitor
for the treatment of sepsis-
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Abstract: Publication date: Available online 4 May 2022Source: European Journal of Medicinal ChemistryAuthor(s): Xuetao Chen, Fanying Meng, Jingtian Zhang, Zijian Zhang, Xuan Ye, Weikun Zhang, Yuanyuan Tong, Xinrui Ji, Rujun Xu, Xiao-Li Xu, Qi-Dong You, Zheng-Yu Jiang
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- Novel hybrid pyrrolidinedione-thiazolidinones as potential anticancer
agents: Synthesis and biological evaluation-
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Abstract: Publication date: Available online 2 May 2022Source: European Journal of Medicinal ChemistryAuthor(s): Nataliya Finiuk, Anna Kryshchyshyn-Dylevych, Serhii Holota, Olga Klyuchivska, Andriy Kozytskiy, Olexandr Karpenko, Nazar Manko, Iryna Ivasechko, Rostyslav Stoika, Roman Lesyk
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- Azetidin-2-one-based small molecules as dual hHDAC6/HDAC8 inhibitors:
Investigation of their mechanism of action and impact of dual inhibition
profile on cell viability-
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Abstract: Publication date: Available online 1 May 2022Source: European Journal of Medicinal ChemistryAuthor(s): Stefano Federico, Tuhina Khan, Anna Fontana, Simone Brogi, Rosaria Benedetti, Federica Sarno, Gabriele Carullo, Alex Pezzotta, Akella Prasanth Saraswati, Eugenia Passaro, Luca Pozzetti, Alessandro Papa, Nicola Relitti, Sandra Gemma, Stefania Butini, Anna Pistocchi, Anna Ramunno, Fabrizio Vincenzi, Katia Varani, Vanessa Tatangelo
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- Design and synthesis of harmiquins, harmine and chloroquine hybrids as
potent antiplasmodial agents-
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Abstract: Publication date: Available online 30 April 2022Source: European Journal of Medicinal ChemistryAuthor(s): Goran Poje, Lais Pessanha de Carvalho, Jana Held, Diana Moita, Miguel Prudêncio, Ivana Perković, Tana Tandarić, Robert Vianello, Zrinka Rajić
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- Targeting EZH2 for cancer therapy: From current progress to novel
strategies-
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Abstract: Publication date: Available online 30 April 2022Source: European Journal of Medicinal ChemistryAuthor(s): Jia Zeng, Jifa Zhang, Ying Sun, Jiaxing Wang, Changyu Ren, Souvik Banerjee, Liang Ouyang, Yuxi Wang
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- Novel bifluorescent Zn(II)–cryptolepine–cyclen complexes trigger
apoptosis induced by nuclear and mitochondrial DNA damage in
cisplatin-resistant lung tumor cells-
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Abstract: Publication date: Available online 30 April 2022Source: European Journal of Medicinal ChemistryAuthor(s): Zhen-Feng Wang, Xiao-Feng Zhou, Qiao-Chang Wei, Qi-Pin Qin, Jin-Xian Li, Ming-Xiong Tan, Shu-Hua Zhang
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- Design, synthesis and antitumor evaluation of novel 1H-indole-2-carboxylic
acid derivatives targeting 14-3-3η protein-
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Abstract: Publication date: Available online 29 April 2022Source: European Journal of Medicinal ChemistryAuthor(s): Zhenxiong Gao, Tingting Fan, Linbo Chen, Mengchu Yang, Vincent Kam Wai Wong, Dawei Chen, Zijian Liu, Yaoyao Zhou, Weibin Wu, Zixuan Qiu, Cunlong Zhang, Yuan Li, Yuyang Jiang
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- Conformational adjustment overcomes multiple drug-resistance mutants of
tropomyosin receptor kinase-
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Abstract: Publication date: 5 July 2022Source: European Journal of Medicinal Chemistry, Volume 237Author(s): Long-Can Mei, Lin-Sheng Zhuo, Hong-Chuang Xu, Wei Huang, Ge-Fei Hao, Guang-Fu Yang
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- Structure-activity relationship and antitumor activity of
-
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Abstract: Publication date: Available online 27 April 2022Source: European Journal of Medicinal ChemistryAuthor(s): Shenyou Nie, Fangrui Wu, Jingyu Wu, Xin Li, Chao Zhou, Yuan Yao, Yongcheng Song
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- Novel non-covalent LSD1 inhibitors endowed with anticancer effects in
leukemia and solid tumor cellular models-
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Abstract: Publication date: Available online 27 April 2022Source: European Journal of Medicinal ChemistryAuthor(s): Martina Menna, Francesco Fiorentino, Biagina Marrocco, Alessia Lucidi, Stefano Tomassi, Domenica Cilli, Mauro Romanenghi, Matteo Cassandri, Silvia Pomella, Michele Pezzella, Donatella Del Bufalo, Mohammad Salik Zeya Ansari, Nevena Tomašević, Milan Mladenović, Monica Viviano, Gianluca Sbardella, Rossella Rota, Daniela Trisciuoglio, Saverio Minucci, Andrea Mattevi
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- Organotropic dendrons with high potency as HIV-1, HIV-2 and EV-A71 cell
entry inhibitors-
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Abstract: Publication date: Available online 27 April 2022Source: European Journal of Medicinal ChemistryAuthor(s): Olaia Martí-Marí, Belén Martínez-Gualda, Irene Fernández-Barahona, Alberto Mills, Rana Abdelnabi, Sam Noppen, Johan Neyts, Dominique Schols, María-José Camarasa, Fernando Herranz, Federico Gago, Ana San-Félix
-
- Halogen substituents enhance oxime nucleophilicity for reactivation of
cholinesterases inhibited by nerve agents-
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Abstract: Publication date: Available online 27 April 2022Source: European Journal of Medicinal ChemistryAuthor(s): Tamara Zorbaz, David Malinak, Tereza Hofmanova, Nikola Maraković, Suzana Žunec, Nikolina Maček Hrvat, Rudolf Andrys, Miroslav Psotka, Antonio Zandona, Jana Svobodova, Lukas Prchal, Sanja Fingler, Maja Katalinić, Zrinka Kovarik, Kamil Musilek
-
- Development of 4-((3-oxo-3-phenylpropyl)amino)benzenesulfonamide
derivatives utilizing tail/dual-tail approaches as novel carbonic
anhydrase inhibitors-
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Abstract: Publication date: Available online 27 April 2022Source: European Journal of Medicinal ChemistryAuthor(s): Mostafa M. Elbadawi, Wagdy M. Eldehna, Alessio Nocentini, Warda R. Somaa, Sara T. Al-Rashood, Eslam B. Elkaeed, Mahmoud A. El Hassab, Hatem A. Abdel-Aziz, Claudiu T. Supuran, Mohamed Fares
-
- Rational design, synthesis and biological evaluation of dual PARP-1/2 and
TNKS1/2 inhibitors for cancer therapy-
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Abstract: Publication date: Available online 27 April 2022Source: European Journal of Medicinal ChemistryAuthor(s): Yizhu Xu, Huanhuan Wu, Lei Huang, Bingxin Zhai, Xiaofei Li, Shuaiqi Xu, Xingxin Wu, Qihua Zhu, Qiang Xu
-
- Similarities and differences between embryonic implantation and CTC
invasion: Exploring the roles of abortifacients in cancer metastasis
chemoprevention-
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Abstract: Publication date: Available online 26 April 2022Source: European Journal of Medicinal ChemistryAuthor(s): Chunlian Zhong, Yusheng Lu, Yumei Li, Huanzhang Xie, Guiyu Zhou, Lee Jia
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- Mechanism of vitamin B6 benzoyl hydrazone platinum(II) complexes overcomes
multidrug resistance in lung cancer-
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Abstract: Publication date: Available online 26 April 2022Source: European Journal of Medicinal ChemistryAuthor(s): Jinxu Qi, Yunyun Zheng, Bin Li, Lai Wei, Jiuling Li, Xiangxiang Xu, Shiru Zhao, Xinhua Zheng, Yihong Wang
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- Optimization of 4-arylthiophene-3-carboxylic acid derivatives as
inhibitors of ANO1: Lead optimization studies toward their analgesic
efficacy for inflammatory pain-
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Abstract: Publication date: Available online 26 April 2022Source: European Journal of Medicinal ChemistryAuthor(s): Yuxi Wang, Xiaoyue Hu, Han Huang, Zefang Jin, Jian Gao, Yi Guo, Yi Zhong, Zhongtang Li, Xiaolin Zong, Kewei Wang, Liangren Zhang, Zhenming Liu
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- New salicylic acid derivatives, double inhibitors of glycolate oxidase and
lactate dehydrogenase, as effective agents decreasing oxalate production-
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Abstract: Publication date: Available online 25 April 2022Source: European Journal of Medicinal ChemistryAuthor(s): Maria Dolores Moya-Garzon, Barbara Rodriguez-Rodriguez, Cristina Martin-Higueras, Francisco Franco-Montalban, Miguel X. Fernandes, Jose A. Gomez-Vidal, Angel L. Pey, Eduardo Salido, Monica Diaz-Gavilan
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- Exploration of 6-methyl-7-(Hetero)Aryl-7-Deazapurine ribonucleosides as
antileishmanial agents-
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Abstract: Publication date: Available online 25 April 2022Source: European Journal of Medicinal ChemistryAuthor(s): Cai Lin, Izet Karalic, An Matheeussen, Pim-Bart Feijens, Fabian Hulpia, Louis Maes, Guy Caljon, Serge Van Calenbergh
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- New Aβ(1–42) ligands from anti-amyloid antibodies: Design, synthesis,
and structural interaction-
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Abstract: Publication date: Available online 23 April 2022Source: European Journal of Medicinal ChemistryAuthor(s): Angelo Santoro, Manuela Grimaldi, Michela Buonocore, Ilaria Stillitano, Antonio Gloria, Matteo Santin, Fabrizio Bobba, Matilde Sublimi Saponetti, Elena Ciaglia, Anna Maria D'Ursi
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- Identification of novel and potent PROTACs targeting FAK for non-small
cell lung cancer: Design, synthesis, and biological study-
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Abstract: Publication date: Available online 23 April 2022Source: European Journal of Medicinal ChemistryAuthor(s): Yin Sun, Ruifeng Wang, Yu Sun, Lin Wang, Yanli Xue, Jingkai Wang, Tianxiao Wu, Wenbo Yin, Qiaohua Qin, Yixiang Sun, Dongmei Zhao, Maosheng Cheng
-
- Recent advances in natural anti-obesity compounds and derivatives based on
in vivo evidence: A mini-review-
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Abstract: Publication date: Available online 22 April 2022Source: European Journal of Medicinal ChemistryAuthor(s): Yi-Han Chang, Hsin-Yi Hung
-
- Discovery of indirubin-3′-aminooxy-acetamide derivatives as potent and
selective FLT3/D835Y mutant kinase inhibitors for acute myeloid leukemia-
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Abstract: Publication date: Available online 21 April 2022Source: European Journal of Medicinal ChemistryAuthor(s): Je-Heon Lee, Ji Eun Shin, WooChan Kim, Pyeonghwa Jeong, Myung Jin Kim, Su Jin Oh, Hyo Jeong Lee, Hyun Woo Park, Sun-Young Han, Yong-Chul Kim
-
- Tapping into the antitubercular potential of 2,5-dimethylpyrroles: A
structure-activity relationship interrogation-
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Abstract: Publication date: Available online 21 April 2022Source: European Journal of Medicinal ChemistryAuthor(s): Dorothy Semenya, Meir Touitou, Domiziana Masci, Camila Maringolo Ribeiro, Fernando Rogerio Pavan, Guilherme Felipe Dos Santos Fernandes, Beatrice Gianibbi, Fabrizio Manetti, Daniele Castagnolo
-
- Discovery of novel non-steroidal selective glucocorticoid receptor
modulators by structure- and IGN-based virtual screening, structural
optimization, and biological evaluation-
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Abstract: Publication date: Available online 20 April 2022Source: European Journal of Medicinal ChemistryAuthor(s): Xueping Hu, Jinping Pang, Changwei Chen, Dejun Jiang, Chao Shen, Xin Chai, Liu Yang, Xujun Zhang, Lei Xu, Sunliang Cui, Tingjun Hou, Dan Li
-
- Synthesis and biological evaluation of geniposide derivatives as
inhibitors of hyperuricemia, inflammatory and fibrosis-
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Abstract: Publication date: Available online 20 April 2022Source: European Journal of Medicinal ChemistryAuthor(s): Jia-shu Chen, Mu-xuan Wang, Min-min Wang, Yu-kai Zhang, Xu Guo, Ying-ying Chen, Meng-qi Zhang, Jin-yue Sun, Yu-fa Liu, Chao Liu
-
- Discovery of novel pleuromutilin derivatives as potent antibacterial
agents-
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Abstract: Publication date: Available online 20 April 2022Source: European Journal of Medicinal ChemistryAuthor(s): Yuhang Zhou, Yunpeng Yi, Jiangkun Wang, Zheng Yang, Qinqin Liu, Wanxia Pu, Ruofeng Shang
-
- Discovery of novel 7,8-dihydropteridine-6(5H)-one-based DNA-PK inhibitors
as potential anticancer agents via scaffold hopping strategy-
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Abstract: Publication date: Available online 20 April 2022Source: European Journal of Medicinal ChemistryAuthor(s): Zongbao Ding, Wei Pan, Yao Xiao, Binbin Cheng, Gang Huang, Jianjun Chen
-
- Occurrence, synthesis and biological activity of 2-(2-phenyethyl)chromones
-
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Abstract: Publication date: Available online 19 April 2022Source: European Journal of Medicinal ChemistryAuthor(s): Meiyan Fan, Wei Yang, Min He, Yongjun Li, Zhiyun Peng, Guangcheng Wang
-
- Potent 2,3-dihydrophthalazine-1,4-dione derivatives as dual inhibitors for
mono-ADP-ribosyltransferases PARP10 and PARP15-
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Abstract: Publication date: Available online 19 April 2022Source: European Journal of Medicinal ChemistryAuthor(s): Maria Giulia Nizi, Mirko M. Maksimainen, Sudarshan Murthy, Serena Massari, Juho Alaviuhkola, Barbara E. Lippok, Sven T. Sowa, Albert Galera-Prat, Renata Prunskaite-Hyyryläinen, Bernhard Lüscher, Patricia Korn, Lari Lehtiö, Oriana Tabarrini
-
- Design, synthesis and antibacterial activity of novel pleuromutilin
derivatives with thieno[2,3-d]pyrimidine substitution-
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Abstract: Publication date: Available online 19 April 2022Source: European Journal of Medicinal ChemistryAuthor(s): Rongcai Ding, Xiaoxia Wang, Jianfang Fu, Yaoyao Chang, Yingxue Li, Yajing Liu, Yue Liu, Jinlong Ma, Jinxing Hu
-
- Application of partially aromatic ortho-quionone-methides for the
synthesis of novel naphthoxazines with improved antibacterial activity-
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Abstract: Publication date: Available online 18 April 2022Source: European Journal of Medicinal ChemistryAuthor(s): Dóra Hegedűs, Nikoletta Szemerédi, Gabriella Spengler, István Szatmári
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- Discovery of small-molecule compounds and natural products against
Parkinson's disease: Pathological mechanism and structural modification-
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Abstract: Publication date: Available online 18 April 2022Source: European Journal of Medicinal ChemistryAuthor(s): Zhichao Zhong, Xingrui He, Jiamin Ge, Junlong Zhu, Chuansheng Yao, Hong Cai, Xiang-Yang Ye, Tian Xie, Renren Bai
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- Insight on pyrimido[5,4-g]indolizine and
pyrimido[4,5-c]pyrrolo[1,2-a]azepine systems as promising photosensitizers
on malignant cells-
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Abstract: Publication date: Available online 18 April 2022Source: European Journal of Medicinal ChemistryAuthor(s): Marilia Barreca, Angela Maria Ingarra, Maria Valeria Raimondi, Virginia Spanò, Michele De Franco, Luca Menilli, Valentina Gandin, Giorgia Miolo, Paola Barraja, Alessandra Montalbano
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- Design, synthesis and biological evaluation of 3-arylisoquinoline
derivatives as topoisomerase I and II dual inhibitors for the therapy of
liver cancer-
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Abstract: Publication date: Available online 18 April 2022Source: European Journal of Medicinal ChemistryAuthor(s): Xuemei Deng, Tian Luo, Xi Zhang, Yuehua Li, Liming Xie, Weifan Jiang, Linyi Liu, Zhen Wang
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- Design, synthesis, and evaluation of a novel series of
mono-indolylbenzoquinones derivatives for the potential treatment of
breast cancer-
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Abstract: Publication date: Available online 16 April 2022Source: European Journal of Medicinal ChemistryAuthor(s): Jingjing Jia, Honglu Yin, Chen Chen, Mingli Hu, Qiu Zhong, Shilong Zheng, Wei Zhang, Haibo Li, Liang Xu, Guangdi Wang, Ling He
-
- Design, synthesis, and biological evaluation of novel diphenylamine
derivatives as tubulin polymerization inhibitors targeting the colchicine
binding site-
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Abstract: Publication date: Available online 16 April 2022Source: European Journal of Medicinal ChemistryAuthor(s): Xiang-Yu Yan, Jia-Fu Leng, Ting-Ting Chen, Yong-Jun Zhao, Ling-Yi Kong, Yong Yin
-
- Discovery and structural optimization of potent epidermal growth factor
receptor (EGFR) inhibitors against L858R/T790M/C797S resistance mutation
for lung cancer treatment-
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Abstract: Publication date: Available online 15 April 2022Source: European Journal of Medicinal ChemistryAuthor(s): Cheng Wang, Xin Wang, Zhi Huang, Tianqi Wang, Yongwei Nie, Shengyong Yang, Rong Xiang, Yan Fan
-
- Synthesis and biological evaluation of conformationally restricted GluN2B
ligands derived from eliprodil-
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Abstract: Publication date: Available online 14 April 2022Source: European Journal of Medicinal ChemistryAuthor(s): Elena Bechthold, Julian A. Schreiber, Nadine Ritter, Dirk Schepmann, Constantin Daniliuc, Guiscard Seebohm, Bernhard Wünsch
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- Structure-based design of novel donepezil-like hybrids for a multi-target
approach to the therapy of Alzheimer's disease-
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Abstract: Publication date: Available online 14 April 2022Source: European Journal of Medicinal ChemistryAuthor(s): Leonardo Brunetti, Rosalba Leuci, Antonio Carrieri, Marco Catto, Sara Occhineri, Giuseppe Vinci, Lucia Gambacorta, Hanna Baltrukevich, Sílvia Chaves, Antonio Laghezza, Cosimo Damiano Altomare, Paolo Tortorella, M. Amélia Santos, Fulvio Loiodice, Luca Piemontese
-
- Convenient PET-tracer production via SuFEx 18F-fluorination of nanomolar
precursor amounts-
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Abstract: Publication date: Available online 14 April 2022Source: European Journal of Medicinal ChemistryAuthor(s): Nils Walter, Jan Bertram, Birte Drewes, Victor Bahutski, Marco Timmer, Markus B. Schütz, Felicia Krämer, Felix Neumaier, Heike Endepols, Bernd Neumaier, Boris D. Zlatopolskiy
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- Structure-activity relationships of 1,4-bis(arylsulfonamido)-benzene or
naphthalene-N,N′-diacetic acids with varying C2-substituents as
inhibitors of Keap1-Nrf2 protein-protein interaction-
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Abstract: Publication date: Available online 13 April 2022Source: European Journal of Medicinal ChemistryAuthor(s): Sumi Lee, Dhulfiqar Ali Abed, Mai-Uyen Nguyen, Michael P. Verzi, Longqin Hu
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- New aldo-keto reductase 1C3 (AKR1C3) inhibitors based on the
hydroxytriazole scaffold-
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Abstract: Publication date: Available online 13 April 2022Source: European Journal of Medicinal ChemistryAuthor(s): Agnese Chiara Pippione, Zühal Kilic-Kurt, Sandra Kovachka, Stefano Sainas, Barbara Rolando, Enrica Denasio, Klaus Pors, Salvatore Adinolfi, Daniele Zonari, Renzo Bagnati, Marco Lucio Lolli, Francesca Spyrakis, Simonetta Oliaro-Bosso, Donatella Boschi
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- The azulene scaffold from a medicinal chemist's perspective:
Physicochemical and in vitro parameters relevant for drug discovery-
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Abstract: Publication date: Available online 12 April 2022Source: European Journal of Medicinal ChemistryAuthor(s): Teppo O. Leino, Peter Sieger, Jari Yli-Kauhaluoma, Erik A.A. Wallén, Jörg T. Kley
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- Semisynthetic pleuromutilin antimicrobials with therapeutic potential
against methicillin-resistant Staphylococcus aureus by targeting 50S
ribosomal subunit-
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Abstract: Publication date: Available online 12 April 2022Source: European Journal of Medicinal ChemistryAuthor(s): Xiao Wang, Rui Wang, Zhao-Sheng Zhang, Guang-Yu Zhang, Zhen Jin, Rong Shen, Dan Du, You-Zhi Tang
-
- The role of the maleimide ring system on the structure-activity
relationship of showdomycin-
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Abstract: Publication date: Available online 11 April 2022Source: European Journal of Medicinal ChemistryAuthor(s): Petja Rosenqvist, Janne J. Mäkinen, Kaisa Palmu, Johanna Jokinen, Ranjit K. Prajapati, Heidi J. Korhonen, Pasi Virta, Georgiy A. Belogurov, Mikko Metsä-Ketelä
-
- Spiral molecules with antimalarial activities: A review
-
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Abstract: Publication date: Available online 8 April 2022Source: European Journal of Medicinal ChemistryAuthor(s): Jing Yang, Yonggang Wang, Wen Guan, Weiwei Su, Gang Li, Suode Zhang, Hongliang Yao
-
- Discovery a series of quinazolin derivatives as potent AXL inhibitors
-
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Abstract: Publication date: Available online 6 April 2022Source: European Journal of Medicinal ChemistryAuthor(s): Lin-Lin Zhang, Jian Wu, Dong-Dong Li, Xiao-Jun Ji, Chang-You Ma, Dan Xu
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- Targeting breast cancer resistance protein (BCRP/ABCG2): Functional
inhibitors and expression modulators-
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Abstract: Publication date: Available online 6 April 2022Source: European Journal of Medicinal ChemistryAuthor(s): Ingrid Fatima Zattoni, Letícia Carani Delabio, Julia de Paula Dutra, Diogo Henrique Kita, Gustavo Scheiffer, Marina Hembecker, Giovana da Silva Pereira, Vivian Rotuno Moure, Glaucio Valdameri
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- Synthesis and pharmacological validation of fluorescent diarylsulfonylurea
analogues as NLRP3 inhibitors and imaging probes-
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Abstract: Publication date: Available online 4 April 2022Source: European Journal of Medicinal ChemistryAuthor(s): Jiannan Zhao, Yongling Li, Jing Ma, Jingting Liu, Ruoxuan Xiao, Linlin Wang, Peng Li, Yinyan He, Feng Qian, Ao Zhang, Zhen-Liang Sun, Chunyong Ding
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- Inhibition of cytochrome P450 monooxygenase catalyzed oxylipin formation
by flavonoids: Evaluation of structure-activity relationship towards
CYP4F2-selective inhibitors-
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Abstract: Publication date: Available online 31 March 2022Source: European Journal of Medicinal ChemistryAuthor(s): Nadja Kampschulte, Tim Berking, Ibrahim E. Çelik, Stefan F. Kirsch, Nils Helge Schebb
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- Synthesis and evaluation of novel HER-2 inhibitors to exert anti-breast
cancer ability through epithelial-mesenchymal transition (EMT) pathway-
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Abstract: Publication date: Available online 29 March 2022Source: European Journal of Medicinal ChemistryAuthor(s): Xin-yang Li, Xin-hua Qian, Ju Zhu, Yu-heng Li, Qi-qi Lin, Shuai Li, Wen-han Xue, Ling-yan Jian, Fan-hao Meng
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- Pep5-based antitumor peptides containing multifunctional fragments with
enhanced activity and synergistic effect-
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Abstract: Publication date: Available online 26 March 2022Source: European Journal of Medicinal ChemistryAuthor(s): Taoran Wang, Long Tian, Qin Cheng, Siliang Feng, Han Zhang, Zhibing Zheng, Yang Liu, Maosheng Cheng, Zhao Meng, Qingbin Meng
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