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Antileishmanial Activity of Pyrazolopyridine Derivatives and Their Potential as an Adjunct Therapy with Miltefosine 

J. Med. Chem. ( IF 5.589 ) 2017-01-20

Devireddy Anand, Pawan Kumar Yadav, Om P. S. Patel, Naveen Parmar, Rahul K. Maurya, Preeti Vishwakarma, Kanumuri S. R. Raju, Isha Taneja, M. Wahajuddin, Susanta Kar, Prem P. Yadav 

Peptide Macrocycle Inhibitor of Coagulation Factor XII with Subnanomolar Affinity and High Target Selectivity 

J. Med. Chem. ( IF 5.589 ) 2017-01-20

Simon J. Middendorp, Jonas Wilbs, Claudia Quarroz, Sara Calzavarini, Anne Angelillo-Scherrer, Christian Heinis 

Pyrimidinyl Biphenylureas: Identification of New Lead Compounds as Allosteric Modulators of the Cannabinoid Receptor CB1 

J. Med. Chem. ( IF 5.589 ) 2017-01-19

Leepakshi Khurana, Bo-Qiao Fu, Anantha L. Duddupudi, Yu-Hsien Liao, Sri Sujana Immadi, Debra A. Kendall, Dai Lu 

Discovery of 2-(((1r,4r)-4-(((4-Chlorophenyl)(phenyl)carbamoyl)oxy)methyl)cyclohexyl)methoxy)acetate (Ralinepag): An Orally Active Prostacyclin Receptor Agonist for the Treatment of Pulmonary Arterial Hypertension 

J. Med. Chem. ( IF 5.589 ) 2017-01-19

Thuy-Anh Tran, Bryan Kramer, Young-Jun Shin, Pureza Vallar, P. Douglas Boatman, Ning Zou, Carleton R. Sage, Tawfik Gharbaoui, Ashwin Krishnan, Biman Pal, Sagar R. Shakya, Antonio Garrido Montalban, John W. Adams, Juan Ramirez, Dominic P. Behan, Anna Shifrina, Anthony Blackburn, Tina Leakakos, Yunqing Shi, Michael Morgan, Abu Sadeque, Weichao Chen, David J. Unett, Ibragim Gaidarov, Xiaohua Chen, Steve Chang, Hsin-Hui Shu, Shiu-Feng Tung, Graeme Semple 

Design, Synthesis, and Biological Evaluation of Small, High-Affinity Siglec-7 Ligands: Toward Novel Inhibitors of Cancer Immune Evasion 

J. Med. Chem. ( IF 5.589 ) 2017-01-19

Horst Prescher, Martin Frank, Stephan Gütgemann, Elena Kuhfeldt, Astrid Schweizer, Lars Nitschke, Carsten Watzl, Reinhard Brossmer 

Potent Inhibition of Nitric Oxide-Releasing Bifendate Derivatives against Drug-Resistant K562/A02 Cells in Vitro and in Vivo 

J. Med. Chem. ( IF 5.589 ) 2017-01-18

Xiaoke Gu, Zhangjian Huang, Zhiguang Ren, Xiaobo Tang, Rongfang Xue, Xiaojun Luo, Sixun Peng, Hui Peng, Bin Lu, Jide Tian, Yihua Zhang 

Structure–Activity Relationship of the Antimalarial Ozonide Artefenomel (OZ439) 

J. Med. Chem. ( IF 5.589 ) 2017-01-18

Yuxiang Dong, Xiaofang Wang, Sriraghavan Kamaraj, Vivek J. Bulbule, Francis C. K. Chiu, Jacques Chollet, Manickam Dhanasekaran, Christopher D. Hein, Petros Papastogiannidis, Julia Morizzi, David M. Shackleford, Helena Barker, Eileen Ryan, Christian Scheurer, Yuanqing Tang, Qingjie Zhao, Lin Zhou, Karen L. White, Heinrich Urwyler, William N. Charman, Hugues Matile, Sergio Wittlin, Susan A. Charman, Jonathan L. Vennerstrom 

Design and Synthesis of Potent and Highly Selective Orexin 1 Receptor Antagonists with a Morphinan Skeleton and Their Pharmacologies 

J. Med. Chem. ( IF 5.589 ) 2017-01-18

Hiroshi Nagase, Naoshi Yamamoto, Masahiro Yata, Sayaka Ohrui, Takahiro Okada, Tsuyoshi Saitoh, Noriki Kutsumura, Yasuyuki Nagumo, Yoko Irukayama-Tomobe, Yukiko Ishikawa, Yasuhiro Ogawa, Shigeto Hirayama, Daisuke Kuroda, Yurie Watanabe, Hiroaki Gouda, Masashi Yanagisawa 

Design of Potent and Selective Cathepsin G Inhibitors Based on the Sunflower Trypsin Inhibitor-1 Scaffold 

J. Med. Chem. ( IF 5.589 ) 2017-01-18

Joakim E. Swedberg, Choi Yi Li, Simon J. de Veer, Conan K. Wang, David J. Craik 

Targeting Type 2 Diabetes with C-Glucosyl Dihydrochalcones as Selective Sodium Glucose Co-Transporter 2 (SGLT2) Inhibitors: Synthesis and Biological Evaluation 

J. Med. Chem. ( IF 5.589 ) 2017-01-18

Ana R. Jesus, Diogo Vila-Viçosa, Miguel Machuqueiro, Ana P. Marques, Timothy M. Dore, Amélia P. Rauter 

A Macrocyclic Agouti-Related Protein/[Nle4,DPhe7]α-Melanocyte Stimulating Hormone Chimeric Scaffold Produces Subnanomolar Melanocortin Receptor Ligands 

J. Med. Chem. ( IF 5.589 ) 2017-01-17

Mark D. Ericson, Katie T. Freeman, Sathya M. Schnell, Carrie Haskell-Luevano 

Design, Synthesis of Novel, Potent, Selective, Orally Bioavailable Adenosine A2A Receptor Antagonists and Their Biological Evaluation 

J. Med. Chem. ( IF 5.589 ) 2017-01-17

Sujay Basu, Dinesh A. Barawkar, Sachin Thorat, Yogesh D. Shejul, Meena Patel, Minakshi Naykodi, Vaibhav Jain, Yogesh Salve, Vandna Prasad, Sumit Chaudhary, Indraneel Ghosh, Ganesh Bhat, Azfar Quraishi, Harish Patil, Shariq Ansari, Suraj Menon, Vishal Unadkat, Rhishikesh Thakare, Madhav S. Seervi, Ashwinkumar V. Meru, Siddhartha De, Ravi K. Bhamidipati, Sreekanth R. Rouduri, Venkata P. Palle, Anita Chug, Kasim A. Mookhtiar 

Tri- and Tetrasubstituted Pyridinylimidazoles as Covalent Inhibitors of c-Jun N-Terminal Kinase 3 

J. Med. Chem. ( IF 5.589 ) 2017-01-17

Felix Muth, Ahmed El-Gokha, Francesco Ansideri, Michael Eitel, Eva Döring, Adrian Sievers-Engler, Andreas Lange, Frank M. Boeckler, Michael Lämmerhofer, Pierre Koch, Stefan A. Laufer 

Discovery of LX2761, a Sodium-Dependent Glucose Cotransporter 1 (SGLT1) Inhibitor Restricted to the Intestinal Lumen, for the Treatment of Diabetes 

J. Med. Chem. ( IF 5.589 ) 2017-01-17

Nicole C. Goodwin, Zhi-Ming Ding, Bryce A. Harrison, Eric D. Strobel, Angela L. Harris, Melinda Smith, Andrea Y. Thompson, Wendy Xiong, Faika Mseeh, Debra J. Bruce, Damaris Diaz, Suma Gopinathan, Ling Li, Emily O’Neill, Mary Thiel, Alan G. E. Wilson, Kenneth G. Carson, David R. Powell, David B. Rawlins 

Difluoromethyl Bioisostere: Examining the “Lipophilic Hydrogen Bond Donor” Concept 

J. Med. Chem. ( IF 5.589 ) 2017-01-17

Yossi Zafrani, Dina Yeffet, Gali Sod-Moriah, Anat Berliner, Dafna Amir, Daniele Marciano, Eytan Gershonov, Sigal Saphier 

N-Heterocyclic (4-Phenylpiperazin-1-yl)methanones Derived from Phenoxazine and Phenothiazine as Highly Potent Inhibitors of Tubulin Polymerization 

J. Med. Chem. ( IF 5.589 ) 2017-01-13

Helge Prinz, Ann-Kathrin Ridder, Kirsten Vogel, Konrad J. Böhm, Igor Ivanov, Jahan B. Ghasemi, Elham Aghaee, Klaus Müller 

Structure-Based Design of Tricyclic NF-κB Inducing Kinase (NIK) Inhibitors That Have High Selectivity over Phosphoinositide-3-kinase (PI3K) 

J. Med. Chem. ( IF 5.589 ) 2017-01-12

Georgette M. Castanedo, Nicole Blaquiere, Maureen Beresini, Brandon Bravo, Hans Brightbill, Jacob Chen, Hai-Feng Cui, Charles Eigenbrot, Christine Everett, Jianwen Feng, Robert Godemann, Emily Gogol, Sarah Hymowitz, Adam Johnson, Nobuhiko Kayagaki, Pawan Bir Kohli, Kathleen Knüppel, Joachim Kraemer, Susan Krüger, Pui Loke, Paul McEwan, Christian Montalbetti, David A. Roberts, Myron Smith, Stefan Steinbacher, Swathi Sujatha-Bhaskar, Ryan Takahashi, Xiaolu Wang, Lawren C. Wu, Yamin Zhang, Steven 

The Essential Medicinal Chemistry of Curcumin 

J. Med. Chem. ( IF 5.589 ) 2017-01-11

Kathryn M. Nelson, Jayme L. Dahlin, Jonathan Bisson, James Graham, Guido F. Pauli, Michael A. Walters 

Design of a Biased Potent Small Molecule Inhibitor of the Bromodomain and PHD Finger-Containing (BRPF) Proteins Suitable for Cellular and in Vivo Studies 

J. Med. Chem. ( IF 5.589 ) 2017-01-09

Niall Igoe, Elliott D. Bayle, Oleg Fedorov, Cynthia Tallant, Pavel Savitsky, Catherine Rogers, Dafydd R. Owen, Gauri Deb, Tim C. P. Somervaille, David M. Andrews, Neil Jones, Anne Cheasty, Hamish Ryder, Paul E. Brennan, Susanne Müller, Stefan Knapp, Paul V. Fish 

Discovery of Novel, Highly Potent, and Selective Matrix Metalloproteinase (MMP)-13 Inhibitors with a 1,2,4-Triazol-3-yl Moiety as a Zinc Binding Group Using a Structure-Based Design Approach 

J. Med. Chem. ( IF 5.589 ) 2017-01-09

Hiroshi Nara, Akira Kaieda, Kenjiro Sato, Takako Naito, Hideyuki Mototani, Hideyuki Oki, Yoshio Yamamoto, Haruhiko Kuno, Takashi Santou, Naoyuki Kanzaki, Jun Terauchi, Osamu Uchikawa, Masakuni Kori 

Discovery of a Potent, Cell Penetrant, and Selective p300/CBP-Associated Factor (PCAF)/General Control Nonderepressible 5 (GCN5) Bromodomain Chemical Probe 

J. Med. Chem. ( IF 5.589 ) 2017-01-09

Philip G. Humphreys, Paul Bamborough, Chun-wa Chung, Peter D. Craggs, Laurie Gordon, Paola Grandi, Thomas G. Hayhow, Jameed Hussain, Katherine L. Jones, Matthew Lindon, Anne-Marie Michon, Jessica F. Renaux, Colin J. Suckling, David F. Tough, Rab K. Prinjha 

Highly Potent and Isoform Selective Dual Site Binding Tankyrase/Wnt Signaling Inhibitors That Increase Cellular Glucose Uptake and Have Antiproliferative Activity 

J. Med. Chem. ( IF 5.589 ) 2017-01-09

Amit Nathubhai, Teemu Haikarainen, Jarkko Koivunen, Sudarshan Murthy, Françoise Koumanov, Matthew D. Lloyd, Geoffrey D. Holman, Taina Pihlajaniemi, David Tosh, Lari Lehtiö, Michael D. Threadgill 

Potent, Selective, Allosteric Inhibition of Human Plasmin by Sulfated Non-Saccharide Glycosaminoglycan Mimetics 

J. Med. Chem. ( IF 5.589 ) 2017-01-05

Daniel K. Afosah, Rami A. Al-Horani, Nehru Viji Sankaranarayanan, Umesh R. Desai 

Toward Understanding the Structural Basis of Partial Agonism at the Dopamine D3 Receptor 

J. Med. Chem. ( IF 5.589 ) 2017-01-05

Mayako Michino, Comfort A. Boateng, Prashant Donthamsetti, Hideaki Yano, Oluyomi M. Bakare, Alessandro Bonifazi, Michael P. Ellenberger, Thomas M. Keck, Vivek Kumar, Clare Zhu, Ravi Verma, Jeffrey R. Deschamps, Jonathan A. Javitch, Amy Hauck Newman, Lei Shi 

Metadynamics for Perspective Drug Design: Computationally Driven Synthesis of New Protein–Protein Interaction Inhibitors Targeting the EphA2 Receptor 

J. Med. Chem. ( IF 5.589 ) 2017-01-05

Matteo Incerti, Simonetta Russo, Donatella Callegari, Daniele Pala, Carmine Giorgio, Ilaria Zanotti, Elisabetta Barocelli, Paola Vicini, Federica Vacondio, Silvia Rivara, Riccardo Castelli, Massimiliano Tognolini, Alessio Lodola 

Structure–Activity Relationships of Small Molecule Autotaxin Inhibitors with a Discrete Binding Mode 

J. Med. Chem. ( IF 5.589 ) 2017-01-05

Lisa M. Miller, Willem-Jan Keune, Diana Castagna, Louise C. Young, Emma L. Duffy, Frances Potjewyd, Fernando Salgado-Polo, Paloma Engel García, Dima Semaan, John M. Pritchard, Anastassis Perrakis, Simon J. F. Macdonald, Craig Jamieson, Allan J. B. Watson 

Discovery of a Highly Potent, Selective, and Metabolically Stable Inhibitor of Receptor-Interacting Protein 1 (RIP1) for the Treatment of Systemic Inflammatory Response Syndrome 

J. Med. Chem. ( IF 5.589 ) 2017-01-05

Yan Ren, Yaning Su, Liming Sun, Sudan He, Lingjun Meng, Daohong Liao, Xiao Liu, Yongfen Ma, Chunyan Liu, Sisi Li, Hanying Ruan, Xiaoguang Lei, Xiaodong Wang, Zhiyuan Zhang 

Design and Synthesis of a Pan-Janus Kinase Inhibitor Clinical Candidate (PF-06263276) Suitable for Inhaled and Topical Delivery for the Treatment of Inflammatory Diseases of the Lungs and Skin 

J. Med. Chem. ( IF 5.589 ) 2017-01-04

Peter Jones, R. Ian Storer, Yogesh A. Sabnis, Florian M. Wakenhut, Gavin A. Whitlock, Katherine S. England, Takasuke Mukaiyama, Christoph M. Dehnhardt, Jotham W. Coe, Steve W. Kortum, Jill E. Chrencik, David G. Brown, Rhys M. Jones, John R. Murphy, Thean Yeoh, Paul Morgan, Iain Kilty 

Structure-Guided Design of EED Binders Allosterically Inhibiting the Epigenetic Polycomb Repressive Complex 2 (PRC2) Methyltransferase 

J. Med. Chem. ( IF 5.589 ) 2017-01-03

Andreas Lingel, Martin Sendzik, Ying Huang, Michael D. Shultz, John Cantwell, Michael P. Dillon, Xingnian Fu, John Fuller, Tobias Gabriel, Justin Gu, Xiangqing Jiang, Ling Li, Fang Liang, Maureen McKenna, Wei Qi, Weijun Rao, Xijun Sheng, Wei Shu, James Sutton, Benjamin Taft, Long Wang, Jue Zeng, Hailong Zhang, Maya Zhang, Kehao Zhao, Mika Lindvall, Dirksen E. Bussiere 

Newly Designed Quinolinol Inhibitors Mitigate the Effects of Botulinum Neurotoxin A in Enzymatic, Cell-Based, and ex Vivo Assays 

J. Med. Chem. ( IF 5.589 ) 2017-01-03

Paul T. Bremer, Michael Adler, Cecilia H. Phung, Ajay K. Singh, Kim D. Janda 

A Versatile Method to Determine the Cellular Bioavailability of Small-Molecule Inhibitors 

J. Med. Chem. ( IF 5.589 ) 2017-01-03

Kevin B. Teuscher, Min Zhang, Haitao Ji 

Discovery of Cell-Permeable O-GlcNAc Transferase Inhibitors via Tethering in Situ Click Chemistry 

J. Med. Chem. ( IF 5.589 ) 2016-12-29

Yue Wang, Jingjing Zhu, Lianwen Zhang 

Disulfide Bond-Containing Ajoene Analogues As Novel Quorum Sensing Inhibitors of Pseudomonas aeruginosa 

J. Med. Chem. ( IF 5.589 ) 2016-12-28

July Fong, Mingjun Yuan, Tim Holm Jakobsen, Kim T. Mortensen, May Margarette Salido Delos Santos, Song Lin Chua, Liang Yang, Choon Hong Tan, Thomas E. Nielsen, Michael Givskov 

Discovery of 2H-Chromen-2-one Derivatives as G Protein-Coupled Receptor-35 Agonists 

J. Med. Chem. ( IF 5.589 ) 2016-12-28

Lai Wei, Jixia Wang, Xiuli Zhang, Ping Wang, Yaopeng Zhao, Jiaqi Li, Tao Hou, Lala Qu, Liying Shi, Xinmiao Liang, Ye Fang 

A Potent, Selective, and Orally Bioavailable HCV NS5A Inhibitor for Treatment of Hepatitis C Virus: (S)-1-((R)-2-(Cyclopropanecarboxamido)-2-phenylacetyl)-N-(4-phenylthiazol-2-yl)pyrrolidine-2-carboxamide 

J. Med. Chem. ( IF 5.589 ) 2016-12-28

Iou-Jiun Kang, Sheng-Ju Hsu, Hui-Yun Yang, Teng-Kuang Yeh, Chung-Chi Lee, Yen-Chun Lee, Ya-Wen Tian, Jen-Shin Song, Tsu-An Hsu, Yu-Sheng Chao, Andrew Yueh, Jyh-Haur Chern 

A Rhodium(III) Complex as an Inhibitor of Neural Precursor Cell Expressed, Developmentally Down-Regulated 8-Activating Enzyme with in Vivo Activity against Inflammatory Bowel Disease 

J. Med. Chem. ( IF 5.589 ) 2016-12-23

Hai-Jing Zhong, Wanhe Wang, Tian-Shu Kang, Hui Yan, Yali Yang, Lipeng Xu, Yuqiang Wang, Dik-Lung Ma, Chung-Hang Leung 

Carbon-11 and Fluorine-18 Radiolabeled Pyridopyrazinone Derivatives for Positron Emission Tomography (PET) Imaging of Phosphodiesterase-5 (PDE5) 

J. Med. Chem. ( IF 5.589 ) 2016-12-23

Rufael Chekol, Olivier Gheysens, Muneer Ahamed, Jan Cleynhens, Peter Pokreisz, Greet Vanhoof, Stefan Janssens, Alfons Verbruggen, Guy Bormans 

Combining Molecular Scaffolds from FDA Approved Drugs: Application to Drug Discovery 

J. Med. Chem. ( IF 5.589 ) 2016-12-23

Richard D. Taylor, Malcolm MacCoss, Alastair D. G. Lawson 

Fatty Acid Cysteamine Conjugates as Novel and Potent Autophagy Activators That Enhance the Correction of Misfolded F508del-Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) 

J. Med. Chem. ( IF 5.589 ) 2016-12-23

Chi B. Vu, Robert J. Bridges, Cecilia Pena-Rasgado, Antonio E. Lacerda, Curtis Bordwell, Abby Sewell, Andrew J. Nichols, Sachin Chandran, Pallavi Lonkar, Dominic Picarella, Amal Ting, Allison Wensley, Maisy Yeager, Feng Liu 

Design and Synthesis of a Series of l-trans-4-Substituted Prolines as Selective Antagonists for the Ionotropic Glutamate Receptors Including Functional and X-ray Crystallographic Studies of New Subtype Selective Kainic Acid Receptor Subtype 1 (GluK1) Anta 

J. Med. Chem. ( IF 5.589 ) 2016-12-22

Niels Krogsgaard-Larsen, Claudia G. Delgar, Karina Koch, Patricia M. G. E. Brown, Charlotte Møller, Liwei Han, Tri H. V. Huynh, Stinne W. Hansen, Birgitte Nielsen, Derek Bowie, Darryl S. Pickering, Jette Sandholm Kastrup, Karla Frydenvang, Lennart Bunch 

Fluorescent Inhibitors as Tools To Characterize Enzymes: Case Study of the Lipid Kinase Phosphatidylinositol 4-Kinase IIIβ (PI4KB) 

J. Med. Chem. ( IF 5.589 ) 2016-12-22

Jana Humpolickova, Ivana Mejdrová, Marika Matousova, Radim Nencka, Evzen Boura 

Rational Design of Novel Highly Potent and Selective Phosphatidylinositol 4-Kinase IIIβ (PI4KB) Inhibitors as Broad-Spectrum Antiviral Agents and Tools for Chemical Biology 

J. Med. Chem. ( IF 5.589 ) 2016-12-22

Ivana Mejdrová, Dominika Chalupská, Pavla Plačková, Christin Müller, Michal Šála, Martin Klíma, Adriana Baumlová, Hubert Hřebabecký, Eliška Procházková, Milan Dejmek, Dmytro Strunin, Jan Weber, Gary Lee, Marika Matoušová, Helena Mertlíková-Kaiserová, John Ziebuhr, Gabriel Birkus, Evzen Boura, Radim Nencka 

Iterative Design and in Vivo Evaluation of an Oncolytic Antilymphoma Peptide 

J. Med. Chem. ( IF 5.589 ) 2016-12-22

J. Johannes Eksteen, Dominik Ausbacher, Jaione Simon-Santamaria, Trine Stiberg, Cristiane Cavalcanti-Jacobsen, Imin Wushur, John S. Svendsen, Øystein Rekdal 

Discovery of a Chemical Probe Bisamide (CCT251236): An Orally Bioavailable Efficacious Pirin Ligand from a Heat Shock Transcription Factor 1 (HSF1) Phenotypic Screen 

J. Med. Chem. ( IF 5.589 ) 2016-12-22

Matthew D. Cheeseman, Nicola E. A. Chessum, Carl S. Rye, A. Elisa Pasqua, Michael J. Tucker, Birgit Wilding, Lindsay E. Evans, Susan Lepri, Meirion Richards, Swee Y. Sharp, Salyha Ali, Martin Rowlands, Lisa O’Fee, Asadh Miah, Angela Hayes, Alan T. Henley, Marissa Powers, Robert te Poele, Emmanuel De Billy, Loredana Pellegrino, Florence Raynaud, Rosemary Burke, Rob L. M. van Montfort, Suzanne A. Eccles, Paul Workman, Keith Jones 

Challenges and Opportunities in the Development of Serine Synthetic Pathway Inhibitors for Cancer Therapy 

J. Med. Chem. ( IF 5.589 ) 2016-12-22

Séverine Ravez, Quentin Spillier, Romain Marteau, Olivier Feron, Raphaël Frédérick 

The Discovery and Hit-to-Lead Optimization of Tricyclic Sulfonamides as Potent and Efficacious Potentiators of Glycine Receptors 

J. Med. Chem. ( IF 5.589 ) 2016-12-21

Howard Bregman, Jeffrey R. Simard, Kristin L. Andrews, Shawn Ayube, Hao Chen, Hakan Gunaydin, Angel Guzman-Perez, Jiali Hu, Liyue Huang, Xin Huang, Paul H. Krolikowski, Sonya G. Lehto, Richard T. Lewis, Klaus Michelsen, Pamela Pegman, Matthew H. Plant, Paul L. Shaffer, Yohannes Teffera, Shuyan Yi, Maosheng Zhang, Jacinthe Gingras, Erin F. DiMauro 

Anticancer and Antiangiogenic Iron(II) Complexes That Target Thioredoxin Reductase to Trigger Cancer Cell Apoptosis 

J. Med. Chem. ( IF 5.589 ) 2016-12-21

Lina Xie, Zuandi Luo, Zhennan Zhao, Tianfeng Chen 

Treatment of Sepsis Pathogenesis with High Mobility Group Box Protein 1-Regulating Anti-inflammatory Agents 

J. Med. Chem. ( IF 5.589 ) 2016-12-21

Wansang Cho, Ja Young Koo, Yeonju Park, Keunhee Oh, Sanghee Lee, Jin-Sook Song, Myung Ae Bae, Donghyun Lim, Dong-Sup Lee, Seung Bum Park 

Structural Basis for Potency and Promiscuity in Poly(ADP-ribose) Polymerase (PARP) and Tankyrase Inhibitors 

J. Med. Chem. ( IF 5.589 ) 2016-12-21

Ann-Gerd Thorsell, Torun Ekblad, Tobias Karlberg, Mirjam Löw, Ana Filipa Pinto, Lionel Trésaugues, Martin Moche, Michael S. Cohen, Herwig Schüler 

Recent Advances in Scaffold Hopping 

J. Med. Chem. ( IF 5.589 ) 2016-12-21

Ye Hu, Dagmar Stumpfe, Jürgen Bajorath 

Synthesis of Novel c(AmpRGD)–Sunitinib Dual Conjugates as Molecular Tools Targeting the αvβ3 Integrin/VEGFR2 Couple and Impairing Tumor-Associated Angiogenesis 

J. Med. Chem. ( IF 5.589 ) 2016-12-20

Andrea Sartori, Elisabetta Portioli, Lucia Battistini, Lido Calorini, Alberto Pupi, Federica Vacondio, Daniela Arosio, Francesca Bianchini, Franca Zanardi 

Aminomethyl-Derived Beta Secretase (BACE1) Inhibitors: Engaging Gly230 without an Anilide Functionality 

J. Med. Chem. ( IF 5.589 ) 2016-12-20

Christopher R. Butler, Kevin Ogilvie, Luis Martinez-Alsina, Gabriela Barreiro, Elizabeth M. Beck, Charles E. Nolan, Kevin Atchison, Eric Benvenuti, Leanne Buzon, Shawn Doran, Cathleen Gonzales, Christopher J. Helal, Xinjun Hou, Mei-Hui Hsu, Eric F. Johnson, Kimberly Lapham, Lorraine Lanyon, Kevin Parris, Brian T. O’Neill, David Riddell, Ashley Robshaw, Felix Vajdos, Michael A. Brodney 

Novel Glycoprotein VI Antagonists as Antithrombotics: Synthesis, Biological Evaluation, and Molecular Modeling Studies on 2,3-Disubstituted Tetrahydropyrido(3,4-b)indoles 

J. Med. Chem. ( IF 5.589 ) 2016-12-20

Shome S. Bhunia, Ankita Misra, Imran A. Khan, Stuti Gaur, Manish Jain, Surendra Singh, Aaruni Saxena, Thomas Hohlfield, Madhu Dikshit, Anil K. Saxena 

Zinc–Metalloproteinase Inhibitors: Evaluation of the Complex Role Played by the Zinc-Binding Group on Potency and Selectivity 

J. Med. Chem. ( IF 5.589 ) 2016-12-20

Cecile Rouanet-Mehouas, Bertrand Czarny, Fabrice Beau, Evelyne Cassar-Lajeunesse, Enrico A. Stura, Vincent Dive, Laurent Devel 

Pyrimidine-Based Inhibitors of Dynamin I GTPase Activity: Competitive Inhibition at the Pleckstrin Homology Domain 

J. Med. Chem. ( IF 5.589 ) 2016-12-20

Luke R. Odell, Mohammed K. Abdel-Hamid, Timothy A. Hill, Ngoc Chau, Kelly A. Young, Fiona M. Deane, Jennette A. Sakoff, Sofia Andersson, James A. Daniel, Phillip J. Robinson, Adam McCluskey 

Triazole Ureas Act as Diacylglycerol Lipase Inhibitors and Prevent Fasting-Induced Refeeding 

J. Med. Chem. ( IF 5.589 ) 2016-12-19

Hui Deng, Sander Kooijman, Adrianus M. C. H. van den Nieuwendijk, Daisuke Ogasawara, Tom van der Wel, Floris van Dalen, Marc P. Baggelaar, Freek J. Janssen, Richard J. B. H. N. van den Berg, Hans den Dulk, Benjamin F. Cravatt, Herman S. Overkleeft, Patrick C. N. Rensen, Mario van der Stelt 

Urea Derivatives of 2-Aryl-benzothiazol-5-amines: A New Class of Potential Drugs for Human African Trypanosomiasis 

J. Med. Chem. ( IF 5.589 ) 2016-12-19

Donald A. Patrick, J. Robert Gillespie, Joshua McQueen, Matthew A. Hulverson, Ranae M. Ranade, Sharon A. Creason, Zackary M. Herbst, Michael H. Gelb, Frederick S. Buckner, Richard R. Tidwell 

When Does Chemical Elaboration Induce a Ligand To Change Its Binding Mode? 

J. Med. Chem. ( IF 5.589 ) 2016-12-16

Shipra Malhotra, John Karanicolas 

Radiolabeled Selective Matrix Metalloproteinase 13 (MMP-13) Inhibitors: (Radio)Syntheses and in Vitro and First in Vivo Evaluation 

J. Med. Chem. ( IF 5.589 ) 2016-12-16

Verena Hugenberg, Stefan Wagner, Klaus Kopka, Michael Schäfers, Robert C. Schuit, Albert D. Windhorst, Sven Hermann 

Some contents have been Reproduced with permission of the American Chemical Society.
Some contents have been Reproduced by permission of The Royal Society of Chemistry.
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