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Emerging New Targets for the Treatment of Resistant Fungal Infections
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.7b01413 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 16, 2018 Category: Chemistry Authors: Na Liu, Jie Tu, Guoqiang Dong, Yan Wang and Chunquan Sheng Source Type: research

Identification of a Potent, Highly Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor Clinical Candidate
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.7b01466 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 16, 2018 Category: Chemistry Authors: Christopher J. Helal, Eric Arnold, Tracey Boyden, Cheng Chang, Thomas A. Chappie, Ethan Fisher, Mihaly Hajos, John F. Harms, William E. Hoffman, John M. Humphrey, Jayvardhan Pandit, Zhijun Kang, Robin J. Kleiman, Bethany L. Kormos, Che-Wah Lee, Jiemin Lu, Source Type: research

Target Identification and Mode of Action of Four Chemically Divergent Drugs against Ebolavirus Infection
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.7b01249 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 16, 2018 Category: Chemistry Authors: Jingshan Ren, Yuguang Zhao, Elizabeth E. Fry and David I. Stuart Source Type: research

Targeting Acidic Mammalian chitinase Is Effective in Animal Model of Asthma
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.7b01051 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 11, 2018 Category: Chemistry Authors: Marzena Mazur, Jacek Olczak, Sylwia Olejniczak, Robert Koralewski, Wojciech Czestkowski, Anna Jedrzejczak, Jakub Golab, Karolina Dzwonek, Barbara Dymek, Piotr L. Sklepkiewicz, Agnieszka Zagozdzon, Tom Noonan, Keyvan Mahboubi, Bruce Conway, Ryan Sheeler, P Source Type: research

Next-Generation Hypoxic Cell Radiosensitizers: Nitroimidazole Alkylsulfonamides
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.7b01678 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 11, 2018 Category: Chemistry Authors: Muriel Bonnet, Cho Rong Hong, Way Wua Wong, Lydia P. Liew, Avik Shome, Jingli Wang, Yongchuan Gu, Ralph J. Stevenson, Wen Qi, Robert F. Anderson, Frederik B. Pruijn, William R. Wilson, Stephen M. F. Jamieson, Kevin O. Hicks and Michael P. Hay Source Type: research

Correction to Synthesis of Potent and Selective Inhibitors of Aldo-Keto Reductase 1B10 and Their Efficacy against Proliferation, Metastasis, and Cisplatin Resistance of Lung Cancer Cells
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.7b01911 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 11, 2018 Category: Chemistry Authors: Satoshi Endo, Shuang Xia, Miho Suyama, Yoshifumi Morikawa, Hiroaki Oguri, Dawei Hu, Yoshinori Ao, Satoyuki Takahara, Yoshikazu Horino, Yoshihiro Hayakawa, Yurie Watanabe, Hiroaki Gouda, Akira Hara, Kazuo Kuwata, Naoki Toyooka, Toshiyuki Matsunaga and Akir Source Type: research

Neutral Porphyrin Derivative Exerts Anticancer Activity by Targeting Cellular Topoisomerase I (Top1) and Promotes Apoptotic Cell Death without Stabilizing Top1-DNA Cleavage Complexes
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.7b01297 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 11, 2018 Category: Chemistry Authors: Subhendu K. Das, Arijit Ghosh, Srijita Paul Chowdhuri, Nyancy Halder, Ishita Rehman, Souvik Sengupta, Krushna Chandra Sahoo, Harapriya Rath and Benu Brata Das Source Type: research

Systematic Tuning of Fluoro-galectin-3 Interactions Provides Thiodigalactoside Derivatives with Single-Digit nM Affinity and High Selectivity
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.7b01626 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 11, 2018 Category: Chemistry Authors: Kristoffer Peterson, Rohit Kumar, Olof Stenstro ̈m, Priya Verma, Prashant R. Verma, Maria Håkansson, Barbro Kahl-Knutsson, Fredrik Zetterberg, Hakon Leffler, Mikael Akke, Derek T. Logan and Ulf J. Nilsson Source Type: research

Fluorescently Labeled Morphine Derivatives for Bioimaging Studies
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.7b01811 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 10, 2018 Category: Chemistry Authors: Raymond Lam, Arisbel B. Gondin, Meritxell Canals, Barrie Kellam, Stephen J. Briddon, Bim Graham and Peter J. Scammells Source Type: research

Discovery of N-(3-Carbamoyl-5,5,7,7-tetramethyl-5,7-dihydro-4H-thieno[2,3-c]pyran-2-yl)-lH-pyrazole-5-carboxamide (GLPG1837), a Novel Potentiator Which Can Open Class III Mutant Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) Channels to a High Extent
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.7b01288 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 10, 2018 Category: Chemistry Authors: Steven E. Van der Plas, Hans Kelgtermans, Tom De Munck, Se ́bastien L. X. Martina, Sébastien Dropsit, Evelyne Quinton, Ann De Blieck, Caroline Joannesse, Linda Tomaskovic, Mia Jans, Thierry Christophe, Ellen van der Aar, Monica Borgonovi, Luc Nelles, M Source Type: research

In Silico Fragment-Based Design Identifies Subfamily B1 Metallo- β-lactamase Inhibitors
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.7b01728 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 10, 2018 Category: Chemistry Authors: Ricky Cain, Ju ̈rgen Brem, David Zollman, Michael A. McDonough, Rachel M. Johnson, James Spencer, Anne Makena, Martine I. Abboud, Samuel Cahill, Sook Y. Lee, Peter J. McHugh, Christopher J. Schofield and Colin W. G. Fishwick Source Type: research

Cyclin-Dependent Kinase 8: A New Hope in Targeted Cancer Therapy?
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.7b00901 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 9, 2018 Category: Chemistry Authors: Stephen Philip, Malika Kumarasiri, Theodosia Teo, Mingfeng Yu and Shudong Wang Source Type: research

Effect of Structural Modifications to Glyoxal-bis(thiosemicarbazonato)copper(II) Complexes on Cellular Copper Uptake, Copper-Mediated ATP7A Trafficking, and P-Glycoprotein Mediated Efflux
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.7b01158 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 8, 2018 Category: Chemistry Authors: Karla M. Acevedo, David J. Hayne, Lachlan E. McInnes, Asif Noor, Clare Duncan, Diane Moujalled, Irene Volitakis, Angela Rigopoulos, Kevin J. Barnham, Victor L. Villemagne, Anthony R. White and Paul S. Donnelly Source Type: research

Quinazolinone-Based Anticancer Agents: Synthesis, Antiproliferative SAR, Antitubulin Activity, and Tubulin Co-crystal Structure
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.7b01474 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 8, 2018 Category: Chemistry Authors: Wolfgang Dohle, Fabrice L. Jourdan, Gre ́gory Menchon, Andrea E. Prota, Paul A. Foster, Pascoe Mannion, Ernest Hamel, Mark P. Thomas, Philip G. Kasprzyk, Eric Ferrandis, Michel O. Steinmetz, Mathew P. Leese and Barry V. L. Potter Source Type: research

Species-Selective Pyrimidineamine Inhibitors of Trypanosoma brucei S-Adenosylmethionine Decarboxylase
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.7b01654 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 5, 2018 Category: Chemistry Authors: Oleg A. Volkov, Anthony J. Brockway, Stephen A. Wring, Michael Peel, Zhe Chen, Margaret A. Phillips and Jef K. De Brabander Source Type: research

Discovery of Novel Selective Acetyl-CoA Carboxylase (ACC) 1 Inhibitors
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.7b01547 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 5, 2018 Category: Chemistry Authors: Ryo Mizojiri, Moriteru Asano, Daisuke Tomita, Hiroshi Banno, Noriyuki Nii, Masako Sasaki, Hiroyuki Sumi, Yoshihiko Satoh, Yukiko Yamamoto, Takeo Moriya, Yoshinori Satomi and Hironobu Maezaki Source Type: research

Demonstrating In-Cell Target Engagement Using a Pirin Protein Degradation Probe (CCT367766)
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.7b01406 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 5, 2018 Category: Chemistry Authors: Nicola E. A. Chessum, Swee Y. Sharp, John J. Caldwell, A. Elisa Pasqua, Birgit Wilding, Giampiero Colombano, Ian Collins, Bugra Ozer, Meirion Richards, Martin Rowlands, Mark Stubbs, Rosemary Burke, P. Craig McAndrew, Paul A. Clarke, Paul Workman, Matthew Source Type: research

“Seriously Sweet”: Acesulfame K Exhibits Selective Inhibition Using Alternative Binding Modes in Carbonic Anhydrase Isoforms
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.7b01470 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 5, 2018 Category: Chemistry Authors: Akilah B. Murray, Carrie L. Lomelino, Claudiu T. Supuran and Robert McKenna Source Type: research

High Mobility Group Box-1 (HMGb1): Current Wisdom and Advancement as a Potential Drug Target
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.7b01136 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 5, 2018 Category: Chemistry Authors: Sonya VanPatten and Yousef Al-Abed Source Type: research

Discovery of LY3104607: A Potent and Selective G Protein-Coupled Receptor 40 (GPR40) Agonist with Optimized Pharmacokinetic Properties to Support Once Daily Oral Treatment in Patients with Type 2 Diabetes Mellitus
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.7b01411 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 5, 2018 Category: Chemistry Authors: Chafiq Hamdouchi, Pranab Maiti, Alan M. Warshawsky, Amy C. DeBaillie, Keith A. Otto, Kelly L. Wilbur, Steven D. Kahl, Anjana Patel Lewis, Guemalli R. Cardona, Richard W. Zink, Keyue Chen, Siddaramaiah CR, Jayana P. Lineswala, Grace L. Neathery, Cecilia Bo Source Type: research

Discovery of Potent and Selective Allosteric Inhibitors of Protein Arginine Methyltransferase 3 (PRMT3)
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.7b01674 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 5, 2018 Category: Chemistry Authors: H. U ̈mit Kaniskan, Mohammad S. Eram, Kehao Zhao, Magdalena M. Szewczyk, Xiaobao Yang, Keith Schmidt, Xiao Luo, Sean Xiao, Miao Dai, Feng He, Irene Zang, Ying Lin, Fengling Li, Elena Dobrovetsky, David Smil, Sun-Joon Min, Jennifer Lin-Jones, Matthieu Sch Source Type: research

Structure-Guided Synthesis and Mechanistic Studies Reveal Sweetspots on Naphthyl Salicyl Hydrazone Scaffold as Non-Nucleosidic Competitive, Reversible Inhibitors of Human Ribonucleotide Reductase
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.7b00530 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 5, 2018 Category: Chemistry Authors: Sarah E. Huff, Faiz Ahmad Mohammed, Mu Yang, Prashansa Agrawal, John Pink, Michael E. Harris, Chris G. Dealwis and Rajesh Viswanathan Source Type: research

Insights into the Impact of a Membrane-Anchoring Moiety on the Biological Activities of Bivalent Compounds As Potential Neuroprotectants for Alzheimer ’s Disease
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.7b01284 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 5, 2018 Category: Chemistry Authors: Liu He, Yuqi Jiang, Kai Liu, Victoria Gomez-Murcia, Xiaopin Ma, Alejandro Torrecillas, Qun Chen, Xiongwei Zhu, Edward Lesnefsky, Juan C. Gomez-Fernandez, Bin Xu and Shijun Zhang Source Type: research

Identification of [18F]TRACK, a Fluorine-18-Labeled Tropomyosin Receptor Kinase (Trk) Inhibitor for PET Imaging
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.7b01607 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 5, 2018 Category: Chemistry Authors: Vadim Bernard-Gauthier, Andrew V. Mossine, Anne Mahringer, Arturo Aliaga, Justin J. Bailey, Xia Shao, Jenelle Stauff, Janna Arteaga, Phillip Sherman, Marilyn Grand ’Maison, Pierre-Luc Rochon, Björn Wängler, Carmen Wängler, Peter Bartenstein, Alexe Source Type: research

Discovery of 4-[(2R,4R)-4-({[1-(2,2-Difluoro-1,3-benzodioxol-5-yl)cyclopropyl]carbonyl}amino)-7-(difluoromethoxy)-3,4-dihydro-2H-chromen-2-yl]benzoic Acid (ABBV/GLPG-2222), a Potent Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) Corrector for the Treatment of Cystic Fibrosis
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.7b01339 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 5, 2018 Category: Chemistry Authors: Xueqing Wang, Bo Liu, Xenia Searle, Clinton Yeung, Andrew Bogdan, Stephen Greszler, Ashvani Singh, Yihong Fan, Andrew M Swensen, Timothy Vortherms, Corina Balut, Ying Jia, Kelly Desino, Wenqing Gao, Hong Yong, Chris Tse and Philip Kym Source Type: research

Structure-Based Design, Synthesis, and In Vivo Antinociceptive Effects of Selective A1 Adenosine Receptor Agonists
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.7b01399 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 3, 2018 Category: Chemistry Authors: Riccardo Petrelli, Mirko Scortichini, Carmela Belardo, Serena Boccella, Livio Luongo, Fabio Capone, Sonja Kachler, Patrizia Vita, Fabio Del Bello, Sabatino Maione, Antonio Lavecchia, Karl-Norbert Klotz and Loredana Cappellacci Source Type: research

High in Vivo Stability of 64Cu-Labeled Cross-Bridged Chelators Is a Crucial Factor in Improved Tumor Imaging of RGD Peptide Conjugates
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.7b01671 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 3, 2018 Category: Chemistry Authors: Swarbhanu Sarkar, Nikunj Bhatt, Yeong Su Ha, Phuong Tu Huynh, Nisarg Soni, Woonghee Lee, Yong Jin Lee, Jung Young Kim, Darpan N. Pandya, Gwang Il An, Kyo Chul Lee, Yongmin Chang and Jeongsoo Yoo Source Type: research

Extra Sugar on Vancomycin: New Analogues for Combating Multidrug-Resistant Staphylococcus aureus and Vancomycin-Resistant Enterococci
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.7b01345 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 2, 2018 Category: Chemistry Authors: Dongliang Guan, Feifei Chen, Lun Xiong, Feng Tang, Faridoon, Yunguang Qiu, Naixia Zhang, Likun Gong, Jian Li, Lefu Lan and Wei Huang Source Type: research

Structure-Based Design of 6-Chloro-4-aminoquinazoline-2-carboxamide Derivatives as Potent and Selective p21-Activated Kinase 4 (PAK4) Inhibitors
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.7b01342 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - December 30, 2017 Category: Chemistry Authors: Chenzhou Hao, Fan Zhao, Hongyan Song, Jing Guo, Xiaodong Li, Xiaolin Jiang, Ran Huan, Shuai Song, Qiaoling Zhang, Ruifeng Wang, Kai Wang, Yu Pang, Tongchao Liu, Tianqi Lu, Wanxu Huang, Jian Wang, Bin Lin, Zhonggui He, Haitao Li, Feng Li, Dongmei Zhao and Source Type: research

From Experiments to a Fast Easy-to-Use Computational Methodology to Predict Human Aldehyde Oxidase Selectivity and Metabolic Reactions
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.7b01552 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - December 29, 2017 Category: Chemistry Authors: Gabriele Cruciani, Nicolo ̀ Milani, Paolo Benedetti, Susan Lepri, Lucia Cesarini, Massimo Baroni, Francesca Spyrakis, Sara Tortorella, Edoardo Mosconi and Laura Goracci Source Type: research

A Stable Heroin Analogue That Can Serve as a Vaccine Hapten to Induce Antibodies That Block the Effects of Heroin and Its Metabolites in Rodents and That Cross-React Immunologically with Related Drugs of Abuse
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.7b01427 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - December 29, 2017 Category: Chemistry Authors: Agnieszka Sulima, Rashmi Jalah, Joshua F. G. Antoline, Oscar B. Torres, Gregory H. Imler, Jeffrey R. Deschamps, Zoltan Beck, Carl R. Alving, Arthur E. Jacobson, Kenner C. Rice and Gary R. Matyas Source Type: research

Targeting Transcriptional Enhanced Associate Domains (TEADs)
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.7b00879 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - December 28, 2017 Category: Chemistry Authors: Floriane Gibault, Manon Sturbaut, Fabrice Bailly, Patricia Melnyk and Philippe Cotelle Source Type: research

Novel Terminal Bipheny-Based Diapophytoene Desaturases (CrtN) Inhibitors as Anti-MRSA/VISR/LRSA Agents with Reduced hERG Activity
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.7b01300 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - December 28, 2017 Category: Chemistry Authors: Baoli Li, Shuaishuai Ni, Fei Mao, Feifei Chen, Yifu Liu, Hanwen Wei, Wenhua Chen, Jin Zhu, Lefu Lan and Jian Li Source Type: research

Inhibit or Evade Multidrug Resistance P-Glycoprotein in Cancer Treatment
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.7b01457 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - December 28, 2017 Category: Chemistry Authors: Deepali Waghray and Qinghai Zhang Source Type: research

Sulfonyl-Containing Boronate Caps for Optimization of Biological Properties of 99mTc(III) Radiotracers [99mTcCl(CDO)(CDOH)2B-R] (CDOH2 = Cyclohexanedione Dioxime)
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.7b01412 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - December 27, 2017 Category: Chemistry Authors: Zuo-Quan Zhao, Min Liu, Wei Fang and Shuang Liu Source Type: research

The Rise and Fall of a Scaffold: A Trend Analysis of Scaffolds in the Medicinal Chemistry Literature
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.7b00954 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - December 27, 2017 Category: Chemistry Authors: Barbara Zdrazil and Rajarshi Guha Source Type: research

Optimization of Orally Bioavailable Enhancer of Zeste Homolog 2 (EZH2) Inhibitors Using Ligand and Property-Based Design Strategies: Identification of Development Candidate (R)-5,8-Dichloro-7-(methoxy(oxetan-3-yl)methyl)-2-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3,4-dihydroisoquinolin-1(2H)-one (PF-06821497)
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.7b01375 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - December 27, 2017 Category: Chemistry Authors: Pei-Pei Kung, Patrick Bingham, Alexei Brooun, Michael Collins, Ya-Li Deng, Dac Dinh, Connie Fan, Ketan S. Gajiwala, Rita Grantner, Hovhannes J. Gukasyan, Wenyue Hu, Buwen Huang, Robert Kania, Susan E. Kephart, Cody Krivacic, Robert A. Kumpf, Penney Khamph Source Type: research

Aniline-Based Inhibitors of Influenza H1N1 Virus Acting on Hemagglutinin-Mediated Fusion
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.7b00908 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - December 22, 2017 Category: Chemistry Authors: Rosana Leiva, Marta Barniol-Xicota, Sandra Codony, Tiziana Ginex, Evelien Vanderlinden, Marta Montes, Michael Caffrey, F. Javier Luque, Lieve Naesens and Santiago Va ́zquez Source Type: research

The Magic of Crystal Structure-Based Inhibitor Optimization: Development of a Butyrylcholinesterase Inhibitor with Picomolar Affinity and in Vivo Activity
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.7b01086 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - December 22, 2017 Category: Chemistry Authors: Urban Kos ̌ak, Boris Brus, Damijan Knez, Simon Žakelj, Jurij Trontelj, Anja Pišlar, Roman Šink, Marko Jukič, Marko Živin, Adrian Podkowa, Florian Nachon, Xavier Brazzolotto, Jure Stojan, Janko Kos, Nicolas Coquelle, Kinga Sałat, Jacques-Philip Source Type: research

Inhibitors of HIV-1 Attachment: The Discovery and Development of Temsavir and its Prodrug Fostemsavir
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.7b01337 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - December 22, 2017 Category: Chemistry Authors: Nicholas A. Meanwell, Mark R. Krystal, Beata Nowicka-Sans, David R. Langley, David A. Conlon, Martin D. Eastgate, Dennis M. Grasela, Peter Timmins, Tao Wang and John F. Kadow Source Type: research

From the Promiscuous Asenapine to Potent Fluorescent Ligands Acting at a Series of Aminergic G-Protein-Coupled Receptors
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.7b01220 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - December 22, 2017 Category: Chemistry Authors: Candide Hounsou, Corinne Baehr, Vincent Gasparik, Doria Alili, Abderazak Belhocine, Thie ́ric Rodriguez, Elodie Dupuis, Thomas Roux, André Mann, Denis Heissler, Jean-Philippe Pin, Thierry Durroux, Dominique Bonnet and Marcel Hibert Source Type: research

Discovery of Peptidomimetic Antibody –Drug Conjugate Linkers with Enhanced Protease Specificity
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.7b01430 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - December 21, 2017 Category: Chemistry Authors: BinQing Wei, Janet Gunzner-Toste, Hui Yao, Tao Wang, Jing Wang, Zijin Xu, Jinhua Chen, John Wai, Jim Nonomiya, Siao Ping Tsai, Josefa Chuh, Katherine R. Kozak, Yichin Liu, Shang-Fan Yu, Jeff Lau, Guangmin Li, Gail D. Phillips, Doug Leipold, Amrita Kamath, Source Type: research

The Design and Development of a Potent and Selective Novel Diprolyl Derivative That Binds to the N-Domain of Angiotensin-I Converting Enzyme
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.7b01478 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - December 21, 2017 Category: Chemistry Authors: Stephen Fienberg, Gyles E. Cozier, K. Ravi Acharya, Kelly Chibale and Edward D. Sturrock Source Type: research

Design of Small Molecule Autophagy Modulators: A Promising Druggable Strategy
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.7b01019 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - December 20, 2017 Category: Chemistry Authors: Siyu He, Qi Li, Xueyang Jiang, Xin Lu, Feng Feng, Wei Qu, Yao Chen and Haopeng Sun Source Type: research

A Dipolar Cycloaddition Reaction To Access 6-Methyl-4,5,6,7-tetrahydro-1H-[1,2,3]triazolo[4,5-c]pyridines Enables the Discovery Synthesis and Preclinical Profiling of a P2X7 Antagonist Clinical Candidate
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.7b01279 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - December 20, 2017 Category: Chemistry Authors: Christa C. Chrovian, Akinola Soyode-Johnson, Alexander A. Peterson, Christine F. Gelin, Xiaohu Deng, Curt A. Dvorak, Nicholas I. Carruthers, Brian Lord, Ian Fraser, Leah Aluisio, Kevin J. Coe, Brian Scott, Tatiana Koudriakova, Freddy Schoetens, Kia Sepass Source Type: research

(+)-Methyl (1R,2S)-2-{[4-(4-Chlorophenyl)-4-hydroxypiperidin-1-yl]methyl}-1-phenylcyclopropanecarboxylate [(+)-MR200] Derivatives as Potent and Selective Sigma Receptor Ligands: Stereochemistry and Pharmacological Properties
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.7b01584 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - December 20, 2017 Category: Chemistry Authors: Emanuele Amata, Antonio Rescifina, Orazio Prezzavento, Emanuela Arena, Maria Dichiara, Valeria Pittala ̀, Ángeles Montilla-García, Francesco Punzo, Pedro Merino, Enrique J. Cobos and Agostino Marrazzo Source Type: research

7-Phenoxy-Substituted 3,4-Dihydro-2H-1,2,4-benzothiadiazine 1,1-Dioxides as Positive Allosteric Modulators of α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptors with Nanomolar Potency
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.7b01323 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - December 19, 2017 Category: Chemistry Authors: Eric Goffin, Thomas Drapier, Anja Probst Larsen, Pierre Geubelle, Christopher P. Ptak, Saara Laulumaa, Karoline Rovinskaja, Julie Gilissen, Pascal de Tullio, Lars Olsen, Karla Frydenvang, Bernard Pirotte, Julien Hanson, Robert E. Oswald, Jette Sandholm Ka Source Type: research

Discovery of Novel Potent VEGFR-2 Inhibitors Exerting Significant Antiproliferative Activity against Cancer Cell Lines
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.7b01091 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - December 19, 2017 Category: Chemistry Authors: Yanmin Zhang, Yadong Chen, Danfeng Zhang, Lu Wang, Tao Lu and Yu Jiao Source Type: research

Alkylated Piperazines and Piperazine-Azole Hybrids as Antifungal Agents
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.7b01138 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - December 19, 2017 Category: Chemistry Authors: Nishad Thamban Chandrika, Sanjib K. Shrestha, Huy X. Ngo, Oleg V. Tsodikov, Kaitlind C. Howard and Sylvie Garneau-Tsodikova Source Type: research

Protac-Induced Protein Degradation in Drug Discovery: Breaking the Rules or Just Making New Ones?
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.7b01272 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - December 19, 2017 Category: Chemistry Authors: Ian Churcher Source Type: research