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Journal of Medicinal Chemistry 
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ISSN (Print) 0022-2623
Published by American Chemical Society (ACS)
[45 journals]
[78 followers] Follow Subscription journalISSN (Print) 0022-2623
Published by American Chemical Society (ACS)
[45 journals]- Design,
Synthesis, and Molecular Modeling of Novel
Pyrido[2,3-d]pyrimidine Analogues As Antifolates;
Application of Buchwald–Hartwig Aminations of Heterocycles
- Authors: Aleem Gangjee; Ojas A. Namjoshi, Sudhir Raghavan, Sherry F. Queener, Roy L. Kisliuk Vivian Cody
Abstract:
Journal of Medicinal Chemistry
DOI : 10.1021/jm400086g
PubDate: 2013-05-21T10:48:32Z
- Authors: Aleem Gangjee; Ojas A. Namjoshi, Sudhir Raghavan, Sherry F. Queener, Roy L. Kisliuk Vivian Cody
- Core Refinement toward Permeable β-Secretase (BACE-1) Inhibitors with Low hERG Activity
- Authors: Tobias Ginman; Jenny Viklund, Jonas Malmström, Jan Blid, Rikard Emond, Rickard Forsblom, Anh Johansson, Annika Kers, Fredrik Lake, Fernando Sehgelmeble, Karin J. Sterky, Margareta Bergh, Anders Lindgren, Patrik Johansson, Fredrik Jeppsson, Johanna Fälting, Ylva Gravenfors Fredrik Rahm
Abstract:
Journal of Medicinal Chemistry
DOI : 10.1021/jm3011349
PubDate: 2013-05-20T11:36:33Z
- Authors: Tobias Ginman; Jenny Viklund, Jonas Malmström, Jan Blid, Rikard Emond, Rickard Forsblom, Anh Johansson, Annika Kers, Fredrik Lake, Fernando Sehgelmeble, Karin J. Sterky, Margareta Bergh, Anders Lindgren, Patrik Johansson, Fredrik Jeppsson, Johanna Fälting, Ylva Gravenfors Fredrik Rahm
- Monitoring
Conformational Changes in Peroxisome Proliferator-Activated
Receptor α by a Genetically Encoded Photoamino Acid, Cross-Linking,
and Mass Spectrometry
- Authors: Rico Schwarz; Dirk Tänzler, Christian H. Ihling, Mathias Q. Müller, Knut Kölbel Andrea Sinz
Abstract:
Journal of Medicinal Chemistry
DOI : 10.1021/jm400446b
PubDate: 2013-05-17T12:01:58Z
- Authors: Rico Schwarz; Dirk Tänzler, Christian H. Ihling, Mathias Q. Müller, Knut Kölbel Andrea Sinz
- X-ray
Crystal Structure of ERK5 (MAPK7) in
Complex with a Specific Inhibitor
- Authors: Jonathan M. Elkins; Jing Wang, Xianming Deng, Michael J. Pattison, J. Simon C. Arthur, Tatiana Erazo, Nestor Gomez, Jose M. Lizcano, Nathanael S. Gray Stefan Knapp
Abstract:
Journal of Medicinal Chemistry
DOI : 10.1021/jm4000837
PubDate: 2013-05-17T11:59:47Z
- Authors: Jonathan M. Elkins; Jing Wang, Xianming Deng, Michael J. Pattison, J. Simon C. Arthur, Tatiana Erazo, Nestor Gomez, Jose M. Lizcano, Nathanael S. Gray Stefan Knapp
- Synthesis,
Pharmacological Characterization, and Docking
Analysis of a Novel Family of Diarylisoxazoles as Highly Selective
Cyclooxygenase-1 (COX-1) Inhibitors
- Authors: Paola Vitale; Stefania Tacconelli, Maria Grazia Perrone, Paola Malerba, Laura Simone, Antonio Scilimati, Antonio Lavecchia, Melania Dovizio, Emanuela Marcantoni, Annalisa Bruno Paola Patrignani
Abstract:
Journal of Medicinal Chemistry
DOI : 10.1021/jm301905a
PubDate: 2013-05-16T20:08:27Z
- Authors: Paola Vitale; Stefania Tacconelli, Maria Grazia Perrone, Paola Malerba, Laura Simone, Antonio Scilimati, Antonio Lavecchia, Melania Dovizio, Emanuela Marcantoni, Annalisa Bruno Paola Patrignani
- Matrix
Metalloproteinase Inhibitors Based on the 3-Mercaptopyrrolidine
Core
- Authors: Yonghao Jin; Mark D. Roycik, Dale B. Bosco, Qiang Cao, Manuel H. Constantino, Martin A. Schwartz Qing-Xiang Amy Sang
Abstract:
Journal of Medicinal Chemistry
DOI : 10.1021/jm400529f
PubDate: 2013-05-16T17:49:18Z
- Authors: Yonghao Jin; Mark D. Roycik, Dale B. Bosco, Qiang Cao, Manuel H. Constantino, Martin A. Schwartz Qing-Xiang Amy Sang
- Xanthates
and Trithiocarbonates Strongly Inhibit Carbonic Anhydrases and Show
Antiglaucoma Effects in Vivo
- Authors: Fabrizio Carta; Atilla Akdemir, Andrea Scozzafava, Emanuela Masini Claudiu T. Supuran
Abstract:
Journal of Medicinal Chemistry
DOI : 10.1021/jm400414j
PubDate: 2013-05-16T13:55:11Z
- Authors: Fabrizio Carta; Atilla Akdemir, Andrea Scozzafava, Emanuela Masini Claudiu T. Supuran
- CROSS:
An Efficient Workflow for Reaction-Driven Rescaffolding
and Side-Chain Optimization Using Robust Chemical Reactions and Available
Reagents
- Authors: Andreas Evers; Gerhard Hessler, Li-hsing Wang, Simon Werrel, Peter Monecke Hans Matter
Abstract:
Journal of Medicinal Chemistry
DOI : 10.1021/jm400404v
PubDate: 2013-05-16T13:53:58Z
- Authors: Andreas Evers; Gerhard Hessler, Li-hsing Wang, Simon Werrel, Peter Monecke Hans Matter
- Hybrid
Molecule from O2-(2,4-Dinitrophenyl)diazeniumdiolate
and Oleanolic Acid: A
Glutathione S-Transferase π-Activated
Nitric Oxide Prodrug with Selective Anti-Human Hepatocellular Carcinoma
Activity and Improved Stability
- Authors: Junjie Fu; Ling Liu, Zhangjian Huang, Yisheng Lai, Hui Ji, Sixun Peng, Jide Tian Yihua Zhang
Abstract:
Journal of Medicinal Chemistry
DOI : 10.1021/jm400393u
PubDate: 2013-05-16T12:52:20Z
- Authors: Junjie Fu; Ling Liu, Zhangjian Huang, Yisheng Lai, Hui Ji, Sixun Peng, Jide Tian Yihua Zhang
- Discovery
of N-{4-[(3-Hydroxyphenyl)-3-methylpiperazin-1-yl]methyl-2-methylpropyl}-4-phenoxybenzamide
Analogues as Selective Kappa Opioid Receptor Antagonists
- Authors: Chad M. Kormos; Chunyang Jin, Juan Pablo Cueva, Scott P. Runyon, James B. Thomas, Lawrence E. Brieaddy, S. Wayne Mascarella, Hernán A. Navarro, Brian P. Gilmour F. Ivy Carroll
Abstract:
Journal of Medicinal Chemistry
DOI : 10.1021/jm400275h
PubDate: 2013-05-16T12:48:43Z
- Authors: Chad M. Kormos; Chunyang Jin, Juan Pablo Cueva, Scott P. Runyon, James B. Thomas, Lawrence E. Brieaddy, S. Wayne Mascarella, Hernán A. Navarro, Brian P. Gilmour F. Ivy Carroll
- Discovery
of Novel STAT3 Small Molecule Inhibitors
via in Silico Site-Directed Fragment-Based Drug Design
- Authors: Wenying Yu; Hui Xiao, Jiayuh Lin Chenglong Li
Abstract:
Journal of Medicinal Chemistry
DOI : 10.1021/jm400080c
PubDate: 2013-05-16T12:47:21Z
- Authors: Wenying Yu; Hui Xiao, Jiayuh Lin Chenglong Li
- Enantioselective
Inhibition of Microbial Lipolytic
Enzymes by Nonracemic Monocyclic Enolphosphonate Analogues of Cyclophostin
- Authors: Vanessa Point; Raj K. Malla, Frederic Carrière, Stéphane Canaan, Christopher D. Spilling Jean-François Cavalier
Abstract:
Journal of Medicinal Chemistry
DOI : 10.1021/jm4000787
PubDate: 2013-05-16T12:45:28Z
- Authors: Vanessa Point; Raj K. Malla, Frederic Carrière, Stéphane Canaan, Christopher D. Spilling Jean-François Cavalier
- Development
and Therapeutic Implications of Selective Histone Deacetylase 6 Inhibitors
- Authors: Jay H. Kalin; Joel A. Bergman
Abstract:
Journal of Medicinal Chemistry
DOI : 10.1021/jm4001659
PubDate: 2013-05-15T12:59:30Z
- Authors: Jay H. Kalin; Joel A. Bergman
- Design,
Synthesis, and Inhibitory Activity of Potent,
Photoswitchable Mast Cell Activation Inhibitors
- Authors: Willem A. Velema; Marco van der Toorn, Wiktor Szymanski Ben L. Feringa
Abstract:
Journal of Medicinal Chemistry
DOI : 10.1021/jm400115k
PubDate: 2013-05-15T12:58:37Z
- Authors: Willem A. Velema; Marco van der Toorn, Wiktor Szymanski Ben L. Feringa
- Fragment-Based
Drug Discovery of 2-Thiazolidinones
as Inhibitors of the Histone Reader BRD4 Bromodomain
- Authors: Lele Zhao; Danyan Cao, Tiantian Chen, Yingqing Wang, Zehong Miao, Yechun Xu, Wuyan Chen, Xin Wang, Yanlian Li, Zhiyan Du, Bing Xiong, Jian Li, Chunyan Xu, Naixia Zhang, Jianhua He Jingkang Shen
Abstract:
Journal of Medicinal Chemistry
DOI : 10.1021/jm301793a
PubDate: 2013-05-14T18:15:00Z
- Authors: Lele Zhao; Danyan Cao, Tiantian Chen, Yingqing Wang, Zehong Miao, Yechun Xu, Wuyan Chen, Xin Wang, Yanlian Li, Zhiyan Du, Bing Xiong, Jian Li, Chunyan Xu, Naixia Zhang, Jianhua He Jingkang Shen
- Novel Adamantyl
Cannabinoids as CB1 Receptor Probes
- Authors: Ganesh A. Thakur; Shama Bajaj, Carol Paronis, Yan Peng, Anna L. Bowman, Lawrence S. Barak, Marc G. Caron, Demon Parrish, Jeffrey R. Deschamps Alexandros Makriyannis
Abstract:
Journal of Medicinal Chemistry
DOI : 10.1021/jm4000775
PubDate: 2013-05-14T15:47:20Z
- Authors: Ganesh A. Thakur; Shama Bajaj, Carol Paronis, Yan Peng, Anna L. Bowman, Lawrence S. Barak, Marc G. Caron, Demon Parrish, Jeffrey R. Deschamps Alexandros Makriyannis
- Small-Molecule
Inhibitors of Cytokine-Mediated STAT1
Signal Transduction in β-Cells with Improved Aqueous
Solubility
- Authors: Stephen S. Scully; Alicia J. Tang, Morten Lundh, Carrie M. Mosher, Kedar M. Perkins Bridget K. Wagner
Abstract:
Journal of Medicinal Chemistry
DOI : 10.1021/jm400397x
PubDate: 2013-05-13T18:24:39Z
- Authors: Stephen S. Scully; Alicia J. Tang, Morten Lundh, Carrie M. Mosher, Kedar M. Perkins Bridget K. Wagner
- Optimization
of Benzoxazole-Based Inhibitors of Cryptosporidium parvum Inosine 5′-Monophosphate Dehydrogenase
- Authors: Suresh Kumar Gorla; Mandapati Kavitha, Minjia Zhang, James En Wai Chin, Xiaoping Liu, Boris Striepen, Magdalena Makowska-Grzyska, Youngchang Kim, Andrzej Joachimiak, Lizbeth Hedstrom Gregory D. Cuny
Abstract:
Journal of Medicinal Chemistry
DOI : 10.1021/jm400241j
PubDate: 2013-05-13T13:05:18Z
- Authors: Suresh Kumar Gorla; Mandapati Kavitha, Minjia Zhang, James En Wai Chin, Xiaoping Liu, Boris Striepen, Magdalena Makowska-Grzyska, Youngchang Kim, Andrzej Joachimiak, Lizbeth Hedstrom Gregory D. Cuny
- Probing
the Role of the Vancomycin E-Ring Aryl
Chloride: Selective Divergent Synthesis and Evaluation of Alternatively
Substituted E-Ring Analogues
- Authors: Joseph R. Pinchman; Dale L. Boger
Abstract:
Journal of Medicinal Chemistry
DOI : 10.1021/jm4004494
PubDate: 2013-05-13T12:20:48Z
- Authors: Joseph R. Pinchman; Dale L. Boger
- Oxadiazole-isopropylamides
as Potent and Noncovalent
Proteasome Inhibitors
- Authors: Sevil Ozcan; Aslamuzzaman Kazi, Frank Marsilio, Bin Fang, Wayne C. Guida, John Koomen, Harshani R. Lawrence Saïd M. Sebti
Abstract:
Journal of Medicinal Chemistry
DOI : 10.1021/jm400221d
PubDate: 2013-05-13T04:56:23Z
- Authors: Sevil Ozcan; Aslamuzzaman Kazi, Frank Marsilio, Bin Fang, Wayne C. Guida, John Koomen, Harshani R. Lawrence Saïd M. Sebti
- Synthesis
and in Vitro and in Vivo Characterization
of Highly β1-Selective β-Adrenoceptor
Partial Agonists
- Authors: Shailesh N. Mistry; Jillian G Baker, Peter M Fischer, Stephen J Hill, Sheila M Gardiner Barrie Kellam
Abstract:
Journal of Medicinal Chemistry
DOI : 10.1021/jm400348g
PubDate: 2013-05-10T20:26:18Z
- Authors: Shailesh N. Mistry; Jillian G Baker, Peter M Fischer, Stephen J Hill, Sheila M Gardiner Barrie Kellam
- Efficacious
Cyclic N-Acyl O-Amino
Phenol
Duocarmycin Prodrugs
- Authors: Amanda L. Wolfe; Katharine K. Duncan, Nikhil K. Parelkar, Douglas Brown, George A. Vielhauer Dale L. Boger
Abstract:
Journal of Medicinal Chemistry
DOI : 10.1021/jm400413r
PubDate: 2013-05-10T20:24:03Z
- Authors: Amanda L. Wolfe; Katharine K. Duncan, Nikhil K. Parelkar, Douglas Brown, George A. Vielhauer Dale L. Boger
- Site-Specific
and Far-Red-Light-Activatable Prodrug
of Combretastatin A-4 Using Photo-Unclick Chemistry
- Authors: Moses Bio; Pallavi Rajaputra, Gregory Nkepang, Samuel G. Awuah, Abugafar M. L. Hossion Youngjae You
Abstract:
Journal of Medicinal Chemistry
DOI : 10.1021/jm400139w
PubDate: 2013-05-10T18:26:13Z
- Authors: Moses Bio; Pallavi Rajaputra, Gregory Nkepang, Samuel G. Awuah, Abugafar M. L. Hossion Youngjae You
- Protein
Kinase Inhibitor Design by Targeting the Asp-Phe-Gly
(DFG) Motif: The Role of the DFG Motif in the Design of Epidermal
Growth Factor Receptor Inhibitors
- Authors: Yi-Hui Peng; Hui-Yi Shiao, Chih-Hsiang Tu, Pang-Min Liu, John Tsu-An Hsu, Prashanth Kumar Amancha, Jian-Sung Wu, Mohane Selvaraj Coumar, Chun-Hwa Chen, Sing-Yi Wang, Wen-Hsing Lin, Hsu-Yi Sun, Yu-Sheng Chao, Ping-Chiang Lyu, Hsing-Pang Hsieh Su-Ying Wu
Abstract:
Journal of Medicinal Chemistry
DOI : 10.1021/jm400072p
PubDate: 2013-05-10T13:39:47Z
- Authors: Yi-Hui Peng; Hui-Yi Shiao, Chih-Hsiang Tu, Pang-Min Liu, John Tsu-An Hsu, Prashanth Kumar Amancha, Jian-Sung Wu, Mohane Selvaraj Coumar, Chun-Hwa Chen, Sing-Yi Wang, Wen-Hsing Lin, Hsu-Yi Sun, Yu-Sheng Chao, Ping-Chiang Lyu, Hsing-Pang Hsieh Su-Ying Wu
- Bifunctional
Inhibition of Human Immunodeficiency
Virus Type 1 Reverse Transcriptase: Mechanism and Proof-of-Concept
as a Novel Therapeutic Design Strategy
- Authors: Christopher M. Bailey; Todd J. Sullivan, Pinar Iyidogan, Julian Tirado-Rives, Raymond Chung, Juliana Ruiz-Caro, Ebrahim Mohamed, William Jorgensen, Roger Hunter Karen S. Anderson
Abstract:
Journal of Medicinal Chemistry
DOI : 10.1021/jm400160s
PubDate: 2013-05-09T20:15:47Z
- Authors: Christopher M. Bailey; Todd J. Sullivan, Pinar Iyidogan, Julian Tirado-Rives, Raymond Chung, Juliana Ruiz-Caro, Ebrahim Mohamed, William Jorgensen, Roger Hunter Karen S. Anderson
- Structure-Based
Approaches to Ligands for G-Protein-Coupled
Adenosine and P2Y Receptors, from Small Molecules to Nanoconjugates
- Authors: Kenneth A. Jacobson
Abstract:
Journal of Medicinal Chemistry
DOI : 10.1021/jm400422s
PubDate: 2013-05-09T20:10:22Z
- Authors: Kenneth A. Jacobson
- Sustainable
Practices in Medicinal Chemistry: Current
State and Future Directions
- Authors: Marian C. Bryan; Barry Dillon, Lawrence G. Hamann, Gregory J. Hughes, Michael E. Kopach, Emily A. Peterson, Mehrnaz Pourashraf, Izzat Raheem, Paul Richardson, Daniel Richter Helen F. Sneddon
Abstract:
Journal of Medicinal Chemistry
DOI : 10.1021/jm400250p
PubDate: 2013-05-09T20:08:56Z
- Authors: Marian C. Bryan; Barry Dillon, Lawrence G. Hamann, Gregory J. Hughes, Michael E. Kopach, Emily A. Peterson, Mehrnaz Pourashraf, Izzat Raheem, Paul Richardson, Daniel Richter Helen F. Sneddon
- Development
of 2′-Substituted (2S,1′R,2′S)-2-(Carboxycyclopropyl)glycine
Analogues as Potent N-Methyl-d-aspartic Acid Receptor
Agonists
- Authors: Rune Risgaard; Simon D. Nielsen, Kasper B. Hansen, Christina M. Jensen, Birgitte Nielsen, Stephen F. Traynelis Rasmus P. Clausen
Abstract:
Journal of Medicinal Chemistry
DOI : 10.1021/jm400346a
PubDate: 2013-05-09T17:01:59Z
- Authors: Rune Risgaard; Simon D. Nielsen, Kasper B. Hansen, Christina M. Jensen, Birgitte Nielsen, Stephen F. Traynelis Rasmus P. Clausen
- Ligand
Based Approach to L-Type Calcium Channel
by Imidazo[2,1-b]thiazole-1,4-Dihydropyridines:
from Heart Activity to Brain Affinity
- Authors: Alessandra Locatelli; Sandro Cosconati, Matteo Micucci, Alberto Leoni, Marinelli Luciana, Andrea Bedini, Pierfranco Ioan, Santi Mario Spampinato, Ettore Novellino, Alberto Chiarini Roberta Budriesi
Abstract:
Journal of Medicinal Chemistry
DOI : 10.1021/jm301839q
PubDate: 2013-05-09T14:09:12Z
- Authors: Alessandra Locatelli; Sandro Cosconati, Matteo Micucci, Alberto Leoni, Marinelli Luciana, Andrea Bedini, Pierfranco Ioan, Santi Mario Spampinato, Ettore Novellino, Alberto Chiarini Roberta Budriesi
- Diastereotopic
and Deuterium Effects in Gemini
- Authors: Hubert Maehr; Natacha Rochel, Hong Jin Lee, Nanjoo Suh Milan R. Uskokovic
Abstract:
Journal of Medicinal Chemistry
DOI : 10.1021/jm400032t
PubDate: 2013-05-09T13:01:29Z
- Authors: Hubert Maehr; Natacha Rochel, Hong Jin Lee, Nanjoo Suh Milan R. Uskokovic
- Biscatecholate–Monohydroxamate
Mixed Ligand Siderophore–Carbacephalosporin Conjugates are
Selective Sideromycin Antibiotics that Target Acinetobacter
baumannii
- Authors: Timothy A. Wencewicz; Marvin J. Miller
Abstract:
Journal of Medicinal Chemistry
DOI : 10.1021/jm400265k
PubDate: 2013-05-08T18:11:24Z
- Authors: Timothy A. Wencewicz; Marvin J. Miller
- Correction
to Systematic in Vivo Screening of a Series of 1-Propyl-4-arylpiperidines
against Dopaminergic and Serotonergic Properties in Rat Brain: A Scaffold-Jumping
Approach
- Authors: Cecilia Mattsson; Theresa Andreasson, Nicholas Waters Clas Sonesson
Abstract: Journal of Medicinal Chemistry
DOI : 10.1021/jm400509x
PubDate: 2013-05-08T14:31:28Z
- Authors: Cecilia Mattsson; Theresa Andreasson, Nicholas Waters Clas Sonesson
- A New Face
for Old Antibiotics: Tetracyclines in Treatment
of Amyloidoses
- Authors: Tatiana Stoilova; Laura Colombo, Gianluigi Forloni, Fabrizio Tagliavini Mario Salmona
Abstract:
Journal of Medicinal Chemistry
DOI : 10.1021/jm400161p
PubDate: 2013-05-08T12:02:19Z
- Authors: Tatiana Stoilova; Laura Colombo, Gianluigi Forloni, Fabrizio Tagliavini Mario Salmona
- A Potent
Bivalent Smac Mimetic (SM-1200) Achieving
Rapid, Complete, and Durable Tumor Regression in Mice
- Authors: Rong Sheng; Haiying Sun, Liu Liu, Jianfeng Lu, Donna McEachern, Guanfeng Wang, Jianfeng Wen, Ping Min, Zhenyun Du, Huirong Lu, Sanmao Kang, Ming Guo, Dajun Yang Shaomeng Wang
Abstract:
Journal of Medicinal Chemistry
DOI : 10.1021/jm400216d
PubDate: 2013-05-07T20:13:04Z
- Authors: Rong Sheng; Haiying Sun, Liu Liu, Jianfeng Lu, Donna McEachern, Guanfeng Wang, Jianfeng Wen, Ping Min, Zhenyun Du, Huirong Lu, Sanmao Kang, Ming Guo, Dajun Yang Shaomeng Wang
- Inhibition
of Rhodesain as a Novel Therapeutic Modality
for Human African Trypanosomiasis
- Authors: Roberta Ettari; Lucia Tamborini, Ilenia C. Angelo, Nicola Micale, Andrea Pinto, Carlo De Micheli Paola Conti
Abstract:
Journal of Medicinal Chemistry
DOI : 10.1021/jm301424d
PubDate: 2013-05-07T19:03:33Z
- Authors: Roberta Ettari; Lucia Tamborini, Ilenia C. Angelo, Nicola Micale, Andrea Pinto, Carlo De Micheli Paola Conti
- Discovery
of a New Class of Natural Product-Inspired
Quinazolinone Hybrid as Potent Antileishmanial agents
- Authors: Moni Sharma; Kuldeep Chauhan, Rahul Shivahare, Preeti Vishwakarma, Manish K. Suthar, Abhisheak Sharma, Suman Gupta, Jitendra K. Saxena, Jawahar Lal, Preeti Chandra, Brijesh Kumar Prem M. S. Chauhan
Abstract:
Journal of Medicinal Chemistry
DOI : 10.1021/jm400053v
PubDate: 2013-05-07T17:06:54Z
- Authors: Moni Sharma; Kuldeep Chauhan, Rahul Shivahare, Preeti Vishwakarma, Manish K. Suthar, Abhisheak Sharma, Suman Gupta, Jitendra K. Saxena, Jawahar Lal, Preeti Chandra, Brijesh Kumar Prem M. S. Chauhan
- Rational
Design and Binding Mode Duality of MDM2–p53
Inhibitors
- Authors: Felix Gonzalez-Lopez de Turiso; Daqing Sun, Yosup Rew, Michael D. Bartberger, Hilary P. Beck, Jude Canon, Ada Chen, David Chow, Tiffany L. Correll, Xin Huang, Lisa D. Julian, Frank Kayser, Mei-Chu Lo, Alexander M. Long, Dustin McMinn, Jonathan D. Oliner, Tao Osgood, Jay P. Powers, Anne Y. Saiki, Steve Schneider, Paul Shaffer, Shou-Hua Xiao, Peter Yakowec, Xuelei Yan, Qiuping Ye, Dongyin Yu, Xiaoning Zhao, Jing Zhou, Julio C. Medina Steven H. Olson
Abstract:
Journal of Medicinal Chemistry
DOI : 10.1021/jm400293z
PubDate: 2013-05-06T20:07:03Z
- Authors: Felix Gonzalez-Lopez de Turiso; Daqing Sun, Yosup Rew, Michael D. Bartberger, Hilary P. Beck, Jude Canon, Ada Chen, David Chow, Tiffany L. Correll, Xin Huang, Lisa D. Julian, Frank Kayser, Mei-Chu Lo, Alexander M. Long, Dustin McMinn, Jonathan D. Oliner, Tao Osgood, Jay P. Powers, Anne Y. Saiki, Steve Schneider, Paul Shaffer, Shou-Hua Xiao, Peter Yakowec, Xuelei Yan, Qiuping Ye, Dongyin Yu, Xiaoning Zhao, Jing Zhou, Julio C. Medina Steven H. Olson
- Design,
Synthesis, and Structure–Activity Relationship
Studies of Novel 3-Alkylindole Derivatives as Selective and
Highly Potent Myeloperoxidase Inhibitors
- Authors: Jalal Soubhye; Iyas Aldib, Betina Elfving, Michel Gelbcke, Paul G. Furtmüller, Manuel Podrecca, Raphaël Conotte, Jean-Marie Colet, Alexandre Rousseau, Florence Reye, Ahmad Sarakbi, Michel Vanhaeverbeek, Jean-Michel Kauffmann, Christian Obinger, Jean Nève, Martine Prévost, Karim Zouaoui Boudjeltia, Francois Dufrasne Pierre Van Antwerpen
Abstract:
Journal of Medicinal Chemistry
DOI : 10.1021/jm4001538
PubDate: 2013-05-06T14:43:03Z
- Authors: Jalal Soubhye; Iyas Aldib, Betina Elfving, Michel Gelbcke, Paul G. Furtmüller, Manuel Podrecca, Raphaël Conotte, Jean-Marie Colet, Alexandre Rousseau, Florence Reye, Ahmad Sarakbi, Michel Vanhaeverbeek, Jean-Michel Kauffmann, Christian Obinger, Jean Nève, Martine Prévost, Karim Zouaoui Boudjeltia, Francois Dufrasne Pierre Van Antwerpen
- Increasing
the Efficiency of Ligands for FK506-Binding
Protein 51 by Conformational Control
- Authors: Yansong Wang; Alexander Kirschner, Anne-Katrin Fabian, Ranganath Gopalakrishnan, Christoph Kress, Bastiaan Hoogeland, Uwe Koch, Christian Kozany, Andreas Bracher Felix Hausch
Abstract:
Journal of Medicinal Chemistry
DOI : 10.1021/jm400087k
PubDate: 2013-05-06T14:30:55Z
- Authors: Yansong Wang; Alexander Kirschner, Anne-Katrin Fabian, Ranganath Gopalakrishnan, Christoph Kress, Bastiaan Hoogeland, Uwe Koch, Christian Kozany, Andreas Bracher Felix Hausch
- Development
of Highly Potent and Selective Diaminothiazole
Inhibitors of Cyclin-Dependent Kinases
- Authors: Ernst Schonbrunn; Stephane Betzi, Riazul Alam, Mathew P. Martin, Andreas Becker, Huijong Han, Rawle Francis, Ramappa Chakrasali, Sudhakar Jakkaraj, Aslamuzzaman Kazi, Said M. Sebti, Christopher L. Cubitt, Anthony W. Gebhard, Lori A. Hazlehurst, Joseph S. Tash Gunda I. Georg
Abstract:
Journal of Medicinal Chemistry
DOI : 10.1021/jm301234k
PubDate: 2013-05-06T14:29:48Z
- Authors: Ernst Schonbrunn; Stephane Betzi, Riazul Alam, Mathew P. Martin, Andreas Becker, Huijong Han, Rawle Francis, Ramappa Chakrasali, Sudhakar Jakkaraj, Aslamuzzaman Kazi, Said M. Sebti, Christopher L. Cubitt, Anthony W. Gebhard, Lori A. Hazlehurst, Joseph S. Tash Gunda I. Georg
- Preliminary
Structure–Activity Relationships and Biological Evaluation
of Novel Antitubercular Indolecarboxamide Derivatives Against Drug-Susceptible
and Drug-Resistant Mycobacterium tuberculosis Strains
- Authors: Oluseye K. Onajole; Marco Pieroni, Suresh K. Tipparaju, Shichun Lun, Jozef Stec, Gang Chen, Hendra Gunosewoyo, Haidan Guo, Nicole C. Ammerman, William R. Bishai Alan P. Kozikowski
Abstract:
Journal of Medicinal Chemistry
DOI : 10.1021/jm4003878
PubDate: 2013-05-03T19:34:28Z
- Authors: Oluseye K. Onajole; Marco Pieroni, Suresh K. Tipparaju, Shichun Lun, Jozef Stec, Gang Chen, Hendra Gunosewoyo, Haidan Guo, Nicole C. Ammerman, William R. Bishai Alan P. Kozikowski
- Kinase
Scaffold Repurposing for Neglected Disease
Drug Discovery: Discovery of an Efficacious, Lapatanib-Derived Lead
Compound for Trypanosomiasis
- Authors: Gautam Patel; Caitlin E. Karver, Ranjan Behera, Paul J. Guyett, Catherine Sullenberger, Peter Edwards, Norma E. Roncal, Kojo Mensa-Wilmot Michael P. Pollastri
Abstract:
Journal of Medicinal Chemistry
DOI : 10.1021/jm400349k
PubDate: 2013-05-03T12:42:33Z
- Authors: Gautam Patel; Caitlin E. Karver, Ranjan Behera, Paul J. Guyett, Catherine Sullenberger, Peter Edwards, Norma E. Roncal, Kojo Mensa-Wilmot Michael P. Pollastri
- β-Secretase
(BACE1) Inhibitors with High
in Vivo Efficacy Suitable for Clinical Evaluation in Alzheimer’s
Disease
- Authors: Hans Hilpert; Wolfgang Guba, Thomas J. Woltering, Wolfgang Wostl, Emmanuel Pinard, Harald Mauser, Alexander V. Mayweg, Mark Rogers-Evans, Roland Humm, Daniela Krummenacher, Thorsten Muser, Christian Schnider, Helmut Jacobsen, Laurence Ozmen, Alessandra Bergadano, David W. Banner, Remo Hochstrasser, Andreas Kuglstatter, Pascale David-Pierson, Holger Fischer, Alessandra Polara Robert Narquizian
Abstract:
Journal of Medicinal Chemistry
DOI : 10.1021/jm400225m
PubDate: 2013-05-02T17:37:42Z
- Authors: Hans Hilpert; Wolfgang Guba, Thomas J. Woltering, Wolfgang Wostl, Emmanuel Pinard, Harald Mauser, Alexander V. Mayweg, Mark Rogers-Evans, Roland Humm, Daniela Krummenacher, Thorsten Muser, Christian Schnider, Helmut Jacobsen, Laurence Ozmen, Alessandra Bergadano, David W. Banner, Remo Hochstrasser, Andreas Kuglstatter, Pascale David-Pierson, Holger Fischer, Alessandra Polara Robert Narquizian
- Pyranoflavones:
A Group of Small-Molecule Probes for Exploring the Active Site Cavities
of Cytochrome P450 Enzymes 1A1, 1A2, and 1B1
- Authors: Jiawang Liu; Shannon F. Taylor, Patrick S. Dupart, Corey L. Arnold, Jayalakshmi Sridhar, Quan Jiang, Yuji Wang, Elena V. Skripnikova, Ming Zhao Maryam Foroozesh
Abstract:
Journal of Medicinal Chemistry
DOI : 10.1021/jm4003654
PubDate: 2013-05-02T12:14:21Z
- Authors: Jiawang Liu; Shannon F. Taylor, Patrick S. Dupart, Corey L. Arnold, Jayalakshmi Sridhar, Quan Jiang, Yuji Wang, Elena V. Skripnikova, Ming Zhao Maryam Foroozesh
- Extreme
Multidrug Resistant HIV-1 Protease
with 20 Mutations Is Resistant to Novel Protease Inhibitors with P1′-Pyrrolidinone
or P2-Tris-tetrahydrofuran
- Authors: Johnson Agniswamy; Chen-Hsiang Shen, Yuan-Fang Wang, Arun K. Ghosh, Kalapala Venkateswara Rao, Chun-Xiao Xu, Jane M. Sayer, John M. Louis Irene T. Weber
Abstract:
Journal of Medicinal Chemistry
DOI : 10.1021/jm400231v
PubDate: 2013-05-01T19:20:09Z
- Authors: Johnson Agniswamy; Chen-Hsiang Shen, Yuan-Fang Wang, Arun K. Ghosh, Kalapala Venkateswara Rao, Chun-Xiao Xu, Jane M. Sayer, John M. Louis Irene T. Weber
- Pyridinylquinazolines
Selectively Inhibit Human Methionine
Aminopeptidase-1 in Cells
- Authors: Feiran Zhang; Shridhar Bhat, Sandra B. Gabelli, Xiaochun Chen, Michelle S. Miller, Benjamin A. Nacev, Yim Ling Cheng, David J. Meyers, Karen Tenney, Joong Sup Shim, Phillip Crews, L. Mario Amzel, Dawei Ma Jun O. Liu
Abstract:
Journal of Medicinal Chemistry
DOI : 10.1021/jm400227z
PubDate: 2013-05-01T19:19:13Z
- Authors: Feiran Zhang; Shridhar Bhat, Sandra B. Gabelli, Xiaochun Chen, Michelle S. Miller, Benjamin A. Nacev, Yim Ling Cheng, David J. Meyers, Karen Tenney, Joong Sup Shim, Phillip Crews, L. Mario Amzel, Dawei Ma Jun O. Liu
- Synthesis
of New Quinolinequinone Derivatives and
Preliminary Exploration of their Cytotoxic Properties
- Authors: Charles M. Keyari; Alison K. Kearns, Nathan S. Duncan, Emily A. Eickholt, Geoffrey Abbott, Howard D. Beall Philippe Diaz
Abstract:
Journal of Medicinal Chemistry
DOI : 10.1021/jm301689x
PubDate: 2013-05-01T14:15:39Z
- Authors: Charles M. Keyari; Alison K. Kearns, Nathan S. Duncan, Emily A. Eickholt, Geoffrey Abbott, Howard D. Beall Philippe Diaz
- Discovery
of the First C-Nucleoside HCV Polymerase Inhibitor
(GS-6620) with Demonstrated Antiviral Response in HCV Infected Patients
- Authors: Aesop Cho; Lijun Zhang, Jie Xu, Rick Lee, Thomas Butler, Sammy Metobo, Vangelis Aktoudianakis, Willard Lew, Hong Ye, Michael Clarke, Edward Doerffler, Daniel Byun, Ting Wang, Darius Babusis, Anne C. Carey, Polina German, Dorothea Sauer, Weidong Zhong, Stephen Rossi, Martijn Fenaux, John G. McHutchison, Jason Perry, Joy Feng, Adrian S. Ray Choung U. Kim
Abstract:
Journal of Medicinal Chemistry
DOI : 10.1021/jm400201a
PubDate: 2013-05-01T11:28:48Z
- Authors: Aesop Cho; Lijun Zhang, Jie Xu, Rick Lee, Thomas Butler, Sammy Metobo, Vangelis Aktoudianakis, Willard Lew, Hong Ye, Michael Clarke, Edward Doerffler, Daniel Byun, Ting Wang, Darius Babusis, Anne C. Carey, Polina German, Dorothea Sauer, Weidong Zhong, Stephen Rossi, Martijn Fenaux, John G. McHutchison, Jason Perry, Joy Feng, Adrian S. Ray Choung U. Kim
- Discovery
of Innovative Therapeutics: Today’s
Realities and Tomorrow’s Vision. 1. Criticisms Faced by the
Pharmaceutical Industry
- Authors: Magid Abou-Gharbia; Wayne E. Childers
Abstract:
Journal of Medicinal Chemistry
DOI : 10.1021/jm400330j
PubDate: 2013-04-29T20:18:39Z
- Authors: Magid Abou-Gharbia; Wayne E. Childers
- Quinoline
Drug–Heme Interactions and Implications
for Antimalarial Cytostatic versus Cytocidal Activities
- Authors: Alexander P. Gorka; Angel de Dios Paul D. Roepe
Abstract:
Journal of Medicinal Chemistry
DOI : 10.1021/jm400282d
PubDate: 2013-04-29T04:09:07Z
- Authors: Alexander P. Gorka; Angel de Dios Paul D. Roepe
- Targeting
Mutant KRAS for Anticancer Therapeutics: A Review of Novel Small Molecule
Modulators
- Authors: Yuanxiang Wang; Christine E. Kaiser, Brendan Frett Hong-yu Li
Abstract:
Journal of Medicinal Chemistry
DOI : 10.1021/jm3017706
PubDate: 2013-04-23T12:33:40Z
- Authors: Yuanxiang Wang; Christine E. Kaiser, Brendan Frett Hong-yu Li
- Hepatitis
C Replication Inhibitors That Target the Viral NS4B Protein
- Authors: John F. Miller; Pek Y. Chong, J. Brad Shotwell, John G. Catalano, Vincent W.-F. Tai, Jing Fang, Anna L. Banka, Christopher D. Roberts, Michael Youngman, Huichang Zhang, Zhiping Xiong, Amanda Mathis, Jeffery J. Pouliot, Robert K. Hamatake, Daniel J. Price, John W. Seal, Lisa L. Stroup, Katrina L. Creech, Luz H. Carballo, Dan Todd, Andrew Spaltenstein, Sylvia Furst, Zhi Hong Andrew J. Peat
Abstract:
Journal of Medicinal Chemistry
DOI : 10.1021/jm400125h
PubDate: 2013-04-19T19:28:23Z
- Authors: John F. Miller; Pek Y. Chong, J. Brad Shotwell, John G. Catalano, Vincent W.-F. Tai, Jing Fang, Anna L. Banka, Christopher D. Roberts, Michael Youngman, Huichang Zhang, Zhiping Xiong, Amanda Mathis, Jeffery J. Pouliot, Robert K. Hamatake, Daniel J. Price, John W. Seal, Lisa L. Stroup, Katrina L. Creech, Luz H. Carballo, Dan Todd, Andrew Spaltenstein, Sylvia Furst, Zhi Hong Andrew J. Peat
- HCV NS5A
Replication Complex Inhibitors. Part 4. Optimization for Genotype 1a Replicon Inhibitory
Activity
- Authors: Denis R. St. Laurent; Michael H. Serrano-Wu, Makonen Belema, Min Ding, Hua Fang, Min Gao, Jason T. Goodrich, Rudolph G. Krause, Julie A. Lemm, Mengping Liu, Omar D. Lopez, Van N. Nguyen, Peter T. Nower, Donald R. O’Boyle, Bradley C. Pearce, Jeffrey L. Romine, Lourdes Valera, Jin-Hua Sun, Ying-Kai Wang, Fukang Yang, Xuejie Yang, Nicholas A. Meanwell Lawrence B. Snyder
Abstract:
Journal of Medicinal Chemistry
DOI : 10.1021/jm301796k
PubDate: 2013-04-10T12:50:05Z
- Authors: Denis R. St. Laurent; Michael H. Serrano-Wu, Makonen Belema, Min Ding, Hua Fang, Min Gao, Jason T. Goodrich, Rudolph G. Krause, Julie A. Lemm, Mengping Liu, Omar D. Lopez, Van N. Nguyen, Peter T. Nower, Donald R. O’Boyle, Bradley C. Pearce, Jeffrey L. Romine, Lourdes Valera, Jin-Hua Sun, Ying-Kai Wang, Fukang Yang, Xuejie Yang, Nicholas A. Meanwell Lawrence B. Snyder
- Orally
Active Opioid Compounds from a Non-Poppy Source
- Authors: Robert B. Raffa; Jaclyn R. Beckett, Vivek N. Brahmbhatt, Theresa M. Ebinger, Chrisjon A. Fabian, Justin R. Nixon, Steven T. Orlando, Chintan A. Rana, Ali H. Tejani Robert J. Tomazic
Abstract:
Journal of Medicinal Chemistry
DOI : 10.1021/jm400143z
PubDate: 2013-04-08T15:51:39Z
- Authors: Robert B. Raffa; Jaclyn R. Beckett, Vivek N. Brahmbhatt, Theresa M. Ebinger, Chrisjon A. Fabian, Justin R. Nixon, Steven T. Orlando, Chintan A. Rana, Ali H. Tejani Robert J. Tomazic
- Therapeutic
Agents Triggering Nonapoptotic Cancer Cell Death
- Authors: Alexander Kornienko; Véronique Mathieu, Shiva K. Rastogi, Florence Lefranc Robert Kiss
Abstract:
Journal of Medicinal Chemistry
DOI : 10.1021/jm400136m
PubDate: 2013-04-05T20:32:10Z
- Authors: Alexander Kornienko; Véronique Mathieu, Shiva K. Rastogi, Florence Lefranc Robert Kiss
- Structure-Based
Design of β-Site APP
Cleaving Enzyme 1 (BACE1) Inhibitors for the Treatment of Alzheimer’s
Disease
- Authors: Jing Yuan; Shankar Venkatraman, Yajun Zheng, Brian M. McKeever, Lawrence W. Dillard Suresh B. Singh
Abstract:
Journal of Medicinal Chemistry
DOI : 10.1021/jm301659n
PubDate: 2013-04-05T17:09:09Z
- Authors: Jing Yuan; Shankar Venkatraman, Yajun Zheng, Brian M. McKeever, Lawrence W. Dillard Suresh B. Singh
- Achiral
Pyrazinone-Based Inhibitors of the Hepatitis
C Virus NS3 Protease and Drug-Resistant Variants with Elongated Substituents
Directed Toward the S2 Pocket
- Authors: Johan Gising; Anna Karin Belfrage, Hiba Alogheli, Angelica Ehrenberg, Eva Åkerblom, Richard Svensson, Per Artursson, Anders Karlén, U. Helena Danielson, Mats Larhed Anja Sandström
Abstract:
Journal of Medicinal Chemistry
DOI : 10.1021/jm301887f
PubDate: 2013-04-02T18:18:25Z
- Authors: Johan Gising; Anna Karin Belfrage, Hiba Alogheli, Angelica Ehrenberg, Eva Åkerblom, Richard Svensson, Per Artursson, Anders Karlén, U. Helena Danielson, Mats Larhed Anja Sandström
- Discovery
of Hepatitis C Virus NS3-4A Protease Inhibitors with Improved Barrier
to Resistance and Favorable Liver Distribution
- Authors: Benoît Moreau; Jeff A. O’Meara, Josée Bordeleau, Michel Garneau, Cedrickx Godbout, Vida Gorys, Mélissa Leblanc, Elisia Villemure, Peter W. White Montse Llinàs-Brunet
Abstract:
Journal of Medicinal Chemistry
DOI : 10.1021/jm400121t
PubDate: 2013-03-28T19:43:31Z
- Authors: Benoît Moreau; Jeff A. O’Meara, Josée Bordeleau, Michel Garneau, Cedrickx Godbout, Vida Gorys, Mélissa Leblanc, Elisia Villemure, Peter W. White Montse Llinàs-Brunet
- Progress
and Developments in Tau Aggregation Inhibitors for Alzheimer Disease
- Authors: Bruno Bulic; Marcus Pickhardt Eckhard Mandelkow
Abstract:
Journal of Medicinal Chemistry
DOI : 10.1021/jm3017317
PubDate: 2013-03-13T20:11:15Z
- Authors: Bruno Bulic; Marcus Pickhardt Eckhard Mandelkow
