[ASAP] Photodynamic Therapy for < italic toggle="yes" > ras < /italic > -Driven Cancers: Targeting G-Quadruplex RNA Structures with Bifunctional Alkyl-Modified Porphyrins
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.9b01577 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 24, 2020 Category: Chemistry Authors: Annalisa Ferino †?, Giulia Nicoletto†?, Francesca D’Este†, Sonia Zorzet‡, Sara Lago§, Sara N. Richter§, Alexander Tikhomirov?, Andrey Shchekotikhin?, and Luigi E. Xodo*† Source Type: research

[ASAP] Discovery and Optimization of Small Molecules Targeting the Protein –Protein Interaction of Heat Shock Protein 90 (Hsp90) and Cell Division Cycle 37 as Orally Active Inhibitors for the Treatment of Colorectal Cancer
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.9b01659 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 24, 2020 Category: Chemistry Authors: Lei Wang †‡, Jingsheng Jiang†‡, Lixiao Zhang†‡, Qiuyue Zhang†‡, Jianrui Zhou†‡, Li Li†‡, Xiaoli Xu*†‡, and Qidong You*†‡ Source Type: research

[ASAP] Discovery and Characterization of Fluorine-Substituted Diarylpyrimidine Derivatives as Novel HIV-1 NNRTIs with Highly Improved Resistance Profiles and Low Activity for the hERG Ion Channel
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.9b01769 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 24, 2020 Category: Chemistry Authors: Dongwei Kang †?, F. Xavier Ruizf|, Da Feng†, Alyssa Pilchf|, Tong Zhao†, Fenju Wei†, Zhao Wang†, Yanying Sun†, Zengjun Fang?, Erik De Clercq§, Christophe Pannecouque§, Eddy Arnold*f|, Xinyong Liu*†, and Peng Zhan*† Source Type: research

[ASAP] Toggling Preassembly with Single-Site Mutation Switches the Cytotoxic Mechanism of Cationic Amphipathic Peptides
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.9b01458 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 23, 2020 Category: Chemistry Authors: Xiaolong Chen †‡, Shuangshuang Ji†‡, Ang Li†‡, Hanjie Liu†‡, and Hao Fei*†‡ Source Type: research

[ASAP] Developing Inhibitors of the p47phox –p22phox Protein–Protein Interaction by Fragment-Based Drug Discovery
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.9b01492 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 23, 2020 Category: Chemistry Authors: Sara Marie Øie Solbak†, Jie Zang†, Dilip Narayanan†, Lars Jakobsen Høj†, Saskia Bucciarelli†, Charlotte Softley‡§, Sebastian Meier?, Annette Eva Langkilde†, Charlotte Held Gotfredsen?, Michael Sattler‡§, and Anders Bach*† Source Type: research

[ASAP] Plasmepsin Inhibitors in Antimalarial Drug Discovery: Medicinal Chemistry and Target Validation (2000 to Present)
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.9b01622 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 23, 2020 Category: Chemistry Authors: Peter Mubanga Cheuka †, Godwin Dziwornu‡, John Okombo§, and Kelly Chibale*‡??# Source Type: research

[ASAP] Development of Novel < italic toggle="yes" > N < /italic > -hydroxypyridone Derivatives as Potential Anti-Ischemic Stroke Agents
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.9b01338 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 22, 2020 Category: Chemistry Authors: Linghao Hu †‡#, Hongxuan Feng§?#, Hongguang Zhang§, Songda Yu?, Qinyuan Zhao§?, Wei Wang§, Fengxia Bao§, Xun Ding§?, Jiajing Hu‡, Manjiong Wang†‡, Yixiang Xu†‡, Zengrui Wu‡, Xiaokang Li†‡, Yun Tang‡, Fei Mao*†‡, Xiaoyan Che Source Type: research

[ASAP] Clobetasol Propionate Is a Heme-Mediated Selective Inhibitor of Human Cytochrome P450 3A5
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.9b02067 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 22, 2020 Category: Chemistry Authors: William C. Wright †‡, Jude Chenge†, Jingheng Wang†, Hazel M. Girvan§, Lei Yang†, Sergio C. Chai†, Andrew D. Huber†, Jing Wu†, Peter O. Oladimeji†, Andrew W. Munro§, and Taosheng Chen*† Source Type: research

[ASAP] Stereoselective Activity of 1-Propargyl-4-styrylpiperidine-like Analogues That Can Discriminate between Monoamine Oxidase Isoforms A and B
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.9b01886 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 22, 2020 Category: Chemistry Authors: Damijan Knez †#, Natalia Colettis‡#, Luca G. Iacovino§#, Matej Sova†, Anja Pis?lar†, Janez Konc?, Samo Les?nik?, Josefina Higgs‡, Fabiola Kamecki‡, Irene Mangialavori‡, Ana Dols?ak†, Simon Z?akelj†, Jurij Trontelj†, Janko Kos†, Clau Source Type: research

[ASAP] < italic toggle="yes" > Mycobacterium tuberculosis < /italic > Decaprenylphosphoryl- ß- < sc > d < /sc > -ribose Oxidase Inhibitors: Expeditious Reconstruction of Suboptimal Hits into a Series with Potent in Vivo Activity
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.9b01561 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 22, 2020 Category: Chemistry Authors: Jennifer A. Borthwick* †?, Carlos Alemparte‡, Ian Wall†, Benjamin C. Whitehurst†?, Argyrides Argyrou†?, Glenn Burley#, Paco de Dios-Anton‡, Laura Guijarro‡, Maria Candida Monteiro‡, Fatima Ortega‡, Colin J Suckling#, Julia Castro Pichel Source Type: research

[ASAP] Dose Predictions for Drug Design
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.9b01365 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 22, 2020 Category: Chemistry Authors: Tristan S. Maurer †, Dennis Smith‡, Kevin Beaumont†, and Li Di*§ Source Type: research

[ASAP] Breaking the Glass Ceiling in Simulation and Modeling: Women in Pharmaceutical Discovery < subtitle > Miniperspective < /subtitle >
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.9b01512 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 22, 2020 Category: Chemistry Authors: Kelly L. Damm-Ganamet †, Renee L. DesJarlais‡, Tami Marrone†, Amy Y. Shih†, Jamie M. Schiffer†, Laura Perez-Benito§, and Taraneh Mirzadegan*† Source Type: research

[ASAP] Drug Annotations for a New Decade
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.0c00036 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 22, 2020 Category: Chemistry Authors: Wendy B. Young(Associate Editor for Drug Annotations, Journal of Medicinal Chemistry), Gunda I. Georg(Editor-in-Chief, Journal of Medicinal Chemistry), and Shaomeng Wang(Editor-in-Chief, Journal of Medicinal Chemistry) Source Type: research

[ASAP] Fragment-to-Lead Medicinal Chemistry Publications in 2018
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.9b01581 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 22, 2020 Category: Chemistry Authors: Daniel A. Erlanson* †, Iwan J. P. de Esch‡, Wolfgang Jahnke§, Christopher N. Johnson?, and Paul N. Mortenson? Source Type: research

[ASAP] Synthesis and Structure –Activity Relationship Studies of C2-Modified Analogs of the Antimycobacterial Natural Product Pyridomycin
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.9b01457 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 21, 2020 Category: Chemistry Authors: Maryline Kienle †?, Patrick Eisenring†?, Barbara Stoessel†?, Oliver P. Horlacher†?, Samuel Hasler†, Gwe´nae¨lle van Colen†, Ruben C. Hartkoorn‡§, Anthony Vocat‡, Stewart T. Cole‡?, and Karl-Heinz Altmann*† Source Type: research

[ASAP] Correction to Antibiotic Adjuvants: Make Antibiotics Great Again!
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.9b02109 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 21, 2020 Category: Chemistry Authors: Hana Douafer, Ve ´ronique Andrieu, Otto Phanstiel, IV, and Jean Michel Brunel* Source Type: research

[ASAP] Comparison of Orexin 1 and Orexin 2 Ligand Binding Modes Using X-ray Crystallography and Computational Analysis
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.9b01787 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 19, 2020 Category: Chemistry Authors: Mathieu Rappas, Ammar A. E. Ali, Kirstie A. Bennett, Jason D. Brown, Sarah J. Bucknell, Miles Congreve, Robert M. Cooke, Gabriella Cseke, Chris de Graaf, Andrew S. Dore ´, James C. Errey†, Ali Jazayeri§, Fiona H. Marshall‡, Jonathan S. Mason, Richar Source Type: research

[ASAP] Systematic Investigation of Lipophilicity Modulation by Aliphatic Fluorination Motifs
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.9b01172 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 17, 2020 Category: Chemistry Authors: Benjamin Jeffries †, Zhong Wang†, Hannah R. Felstead†, Jean-Yves Le Questel‡, James S. Scott§, Elisabetta Chiarparin§, Je´ro^me Graton*‡, and Bruno Linclau*† Source Type: research

[ASAP] Discovery of Balovaptan, a Vasopressin 1a Receptor Antagonist for the Treatment of Autism Spectrum Disorder
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.9b01478 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 17, 2020 Category: Chemistry Authors: Patrick Schnider*, Caterina Bissantz, Andreas Bruns, Cosimo Dolente, Erwin Goetschi, Roland Jakob-Roetne, Basil Ku ¨nnecke, Thomas Mueggler, Wolfgang Muster, Neil Parrott, Emmanuel Pinard, Hasane Ratni, Ce´line Risterucci, Mark Rogers-Evans, Markus von Source Type: research

[ASAP] Potent, Selective, Water Soluble, Brain-Permeable EP2 Receptor Antagonist for Use in Central Nervous System Disease Models
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.9b01218 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 16, 2020 Category: Chemistry Authors: Radhika Amaradhi, Avijit Banik, Shabber Mohammed, Vidyavathi Patro, Asheebo Rojas, Wenyi Wang, Damoder Reddy Motati, Ray Dingledine, and Thota Ganesh* Source Type: research

[ASAP] Computational Method for Structure-Based Analysis of SAR Transfer
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.9b01931 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 15, 2020 Category: Chemistry Authors: Davide Bonanni †‡, Marco L. Lolli†, and Ju¨rgen Bajorath*‡ Source Type: research

[ASAP] The Discovery of 7-Methyl-2-[(7-methyl[1,2,4]triazolo[1,5- < italic toggle="yes" > a < /italic > ]pyridin-6-yl)amino]-9-(tetrahydro-2 < italic toggle="yes" > H < /italic > -pyran-4-yl)-7,9-dihydro-8 < italic toggle="yes" > H < /italic > -purin-8-one (AZD7648), a Potent and Selective DNA-Dependent Protein Kinase (DNA-PK) Inhibitor
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.9b01684 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 15, 2020 Category: Chemistry Authors: Frederick W. Goldberg* †, M. Raymond V. Finlay†, Attilla K. T. Ting†, David Beattie†, Gillian M. Lamont†, Charlene Fallan†, Gail L. Wrigley†, Marianne Schimpl‡, Martin R. Howard†, Beth Williamson†, Mercedes Vazquez-Chantada‡, Derek G Source Type: research

[ASAP] Discovery of a Novel, Highly Potent, and Selective Thieno[3,2- < italic toggle="yes" > d < /italic > ]pyrimidinone-Based Cdc7 Inhibitor with a Quinuclidine Moiety (TAK-931) as an Orally Active Investigational Antitumor Agent
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.9b01427 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 14, 2020 Category: Chemistry Authors: Osamu Kurasawa* †?, Tohru Miyazaki†, Misaki Homma†, Yuya Oguro†, Takashi Imada†, Noriko Uchiyama†, Kenichi Iwai†, Yukiko Yamamoto†, Momoko Ohori†, Hideto Hara†, Hiroshi Sugimoto†, Kentaro Iwata‡, Robert Skene§, Isaac Hoffman§, Ak Source Type: research

[ASAP] Discovery of Potent and Selective Epidermal Growth Factor Receptor (EGFR) Bifunctional Small-Molecule Degraders
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.9b01566 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 14, 2020 Category: Chemistry Authors: Meng Cheng †‡#, Xufen Yu*?#, Kaylene Lu‡, Ling Xie§, Li Wang§, Fanye Meng?, Xiaoran Han‡?, Xian Chen§, Jing Liu?, Yue Xiong*‡†§, and Jian Jin*? Source Type: research

[ASAP] Heterobifunctional Molecules Induce Dephosphorylation of Kinases –A Proof of Concept Study
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.9b01167 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 14, 2020 Category: Chemistry Authors: Sayumi Yamazoe* †?, Jeffrey Tom‡, Yue Fu‡, Wenqiong Wu?, Liang Zeng?, Changlei Sun?, Qi Liu?, Jie Lin§, Kui Lin§, Wayne J. Fairbrother‡, and Steven T. Staben*† Source Type: research

[ASAP] Novel Class of Colony-Stimulating Factor 1 Receptor Kinase Inhibitors Based on an < italic toggle="yes" > o < /italic > -Aminopyridyl Alkynyl Scaffold as Potential Treatment for Inflammatory Disorders
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.9b01912 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 14, 2020 Category: Chemistry Authors: Zhicheng Xie †§?, Bing Wu‡§?, Yingqiang Liu†??, Wenming Ren†, Linjiang Tong†§, Caigui Xiang‡§, Aihuan Wei†, Yuanzhuo Gao‡§, Limin Zeng†, Hua Xie*†§, Wei Tang*‡§, and Youhong Hu*†§ Source Type: research

[ASAP] Synthesis and Biological Evaluation of B-Cell Lymphoma 6 Inhibitors of < italic toggle="yes" > N < /italic > -Phenyl-4-pyrimidinamine Derivatives Bearing Potent Activities against Tumor Growth
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.9b01618 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 13, 2020 Category: Chemistry Authors: Weikai Guo †§, Yajing Xing†§, Qiansen Zhang†, Jiuqing Xie†, Dongxia Huang†, Haijun Gu†, Peng He†, Miaoran Zhou‡, Shifen Xu‡, Xiufeng Pang†, Mingyao Liu*†, Zhengfang Yi*†, and Yihua Chen*† Source Type: research

[ASAP] Docking Finds GPCR Ligands in Dark Chemical Matter
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.9b01560 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 13, 2020 Category: Chemistry Authors: Flavio Ballante †#, Axel Rudling‡#, Alexey Zeifman†‡#, Andreas Luttens†, Duy Duc Vo†, John J. Irwin§, Jan Kihlberg?, Jose Brea?, Maria Isabel Loza?, and Jens Carlsson*† Source Type: research

[ASAP] Scaffold Hopping of Natural Product Evodiamine: Discovery of a Novel Antitumor Scaffold with Excellent Potency against Colon Cancer
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.9b01626 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 10, 2020 Category: Chemistry Authors: Lei Wang †‡, Kun Fang†, Junfei Cheng†, Yu Li†, Yahui Huang†, Shuqiang Chen†, Guoqiang Dong*†, Shanchao Wu*†, and Chunquan Sheng*†‡§ Source Type: research

[ASAP] Discovery of BAY-985, a Highly Selective TBK1/IKKe Inhibitor
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.9b01460 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 10, 2020 Category: Chemistry Authors: Julien Lefranc* †, Volker Klaus Schulze†, Roman Christian Hillig†, Hans Briem†, Florian Prinz†, Anne Mengel†, Tobias Heinrich†, Jozsef Balint‡, Srinivasan Rengachari§?, Horst Irlbacher†, Detlef Sto¨ckigt†, Ulf Bo¨mer†, Benjamin Ba Source Type: research

[ASAP] Binding Loop Substitutions in the Cyclic Peptide SFTI-1 Generate Potent and Selective Chymase Inhibitors
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.9b01811 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 9, 2020 Category: Chemistry Authors: Choi Yi Li, Kuok Yap, Joakim E. Swedberg, David J. Craik, and Simon J. de Veer* Source Type: research

[ASAP] Subtype-Selective Fluorescent Ligands as Pharmacological Research Tools for the Human Adenosine A < sub > 2A < /sub > Receptor
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.9b01856 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 9, 2020 Category: Chemistry Authors: Eleonora Comeo †§?, Nicholas D. Kindon†§, Mark Soave‡§, Leigh A. Stoddart‡§, Laura E. Kilpatrick‡§, Peter J. Scammells?, Stephen J. Hill*‡§, and Barrie Kellam*†§ Source Type: research

[ASAP] Selectivity and Physicochemical Optimization of Repurposed Pyrazolo[1,5- < italic toggle="yes" > b < /italic > ]pyridazines for the Treatment of Human African Trypanosomiasis
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.9b01741 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 8, 2020 Category: Chemistry Authors: Westley F. Tear †, Seema Bag†, Rosario Diaz-Gonzalez‡, Gloria Ceballos-Pe´rez‡, Domingo I. Rojas-Barros‡, Carlos Cordon-Obras‡?, Guiomar Pe´rez-Moreno‡, Raquel Garci´a-Herna´ndez‡, Maria Santos Martinez-Martinez§, Luis Miguel Ruiz-Per Source Type: research

[ASAP] Optimization of Orally Bioavailable PI3Kd Inhibitors and Identification of Vps34 as a Key Selectivity Target
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.9b01585 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 8, 2020 Category: Chemistry Authors: Zoe ¨ A. Henley*†, Augustin Amour±, Nick Barton§, Marcus Bantscheff?, Giovanna Bergamini?, Sophie M. Bertrand†, Ma´ire Convery‡, Kenneth Down†, Birgit Du¨mpelfeld?, Chris D. Edwards?, Paola Grandi?, Paul M. Gore†, Steve Keeling†, Stefano Source Type: research

[ASAP] Identification of Selective Inhibitors of < italic toggle="yes" > Plasmodium < /italic > N-Myristoyltransferase by High-Throughput Screening
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.9b01343 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 8, 2020 Category: Chemistry Authors: Anke Harupa †‡§, Laura De Las Heras‡, Gonzalo Colmenarejo‡?, Sally Lyons-Abbott†? & , Alexandra Reers †??, Iva´n Caballero Hernandez‡?, Chun-Wa Chung‡, David Charter‡, Peter J. Myler†??, Raquel M. Ferna´ndez-Mene´ndez‡, Fe´lix C Source Type: research

[ASAP] Structure –Activity Relationship Study of Novel 6-Aryl-2-benzoyl-pyridines as Tubulin Polymerization Inhibitors with Potent Antiproliferative Properties
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.9b01815 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 7, 2020 Category: Chemistry Authors: Hao Chen †?, Shanshan Deng†?, Yuxi Wang‡?, Najah Albadari†, Gyanendra Kumar§, Dejian Ma†, Weimin Li‡, Stephen W. White§, Duane D. Miller†, and Wei Li*† Source Type: research

[ASAP] Synthesis and in Vitro and in Vivo Biological Evaluation of Tissue-Specific Bisthiazole Histone Deacetylase (HDAC) Inhibitors
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.9b01792 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 7, 2020 Category: Chemistry Authors: Shu-Wei Zhang †?, Chao-Jun Gong†, Ming-Bo Su†, Fei Chen†, Ting He§, Yang-Ming Zhang†‡, Qian-Qian Shen§, Yi Su§, Jian Ding§, Jia Li*†, Yi Chen*§, and Fa-Jun Nan*†‡ Source Type: research

[ASAP] Potent Thiophene Antagonists of Human Complement C3a Receptor with Anti-Inflammatory Activity
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.9b00927 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 7, 2020 Category: Chemistry Authors: Jessica A. Rowley †‡?, Robert C. Reid*†‡§?, Eunice K. Y. Poon†§?, Kai-Chen Wu†‡§, Junxian Lim†‡§, Rink-Jan Lohman†‡§, Johan K. Hamidon†, Mei-Kwan Yau†, Maria A. Halili†‡, Thomas Durek†, Abishek Iyer†‡§, and David Source Type: research

[ASAP] Discovery and Structure-Based Optimization of Potent and Selective WD Repeat Domain 5 (WDR5) Inhibitors Containing a Dihydroisoquinolinone Bicyclic Core
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.9b01608 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 7, 2020 Category: Chemistry Authors: Jianhua Tian#, Kevin B. Teuscher †, Erin R. Aho‡, Joseph R. Alvarado†, Jonathan J. Mills†, Kenneth M. Meyers†, Rocco D. Gogliotti†, Changho Han†, Jonathan D. Macdonald†, Jiqing Sai†, J. Grace Shaw†, John L. Sensintaffar†, Bin Zhao† Source Type: research

[ASAP] Stepwise Evolution of Fragment Hits against MAPK Interacting Kinases 1 and 2
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.9b01582 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 7, 2020 Category: Chemistry Authors: Jacek Kwiatkowski, Boping Liu, Shermaine Pang, Nur Huda Binte Ahmad, Gang Wang, Anders Poulsen, Haiyan Yang, Yong Rui Poh, Doris Hui Ying Tee, Esther Ong, Priya Retna, Nurul Dinie, Perlyn Kwek, John Liang Kuan Wee, Vithya Manoharan, Choon Bing Low, Peck G Source Type: research

[ASAP] Incorporation of Agouti-Related Protein (AgRP) Human Single Nucleotide Polymorphisms (SNPs) in the AgRP-Derived Macrocyclic Scaffold c[Pro-Arg-Phe-Phe-Asn-Ala-Phe- < sc > d < /sc > Pro] Decreases Melanocortin-4 Receptor Antagonist Potency and Results in the Discovery of Melanocortin-5 Receptor Antagonists
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.9b00860 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 6, 2020 Category: Chemistry Authors: Zoe M. Koerperich †, Mark D. Ericson†, Katie T. Freeman†, Robert C. Speth‡§, Irina D. Pogozheva?, Henry I. Mosberg?, and Carrie Haskell-Luevano*† Source Type: research

[ASAP] Discovery of a Bromodomain and Extraterminal Inhibitor with a Low Predicted Human Dose through Synergistic Use of Encoded Library Technology and Fragment Screening
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.9b01670 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 6, 2020 Category: Chemistry Authors: Christopher R. Wellaway* †, Dominique Amans†, Paul Bamborough†, Heather Barnett†, Rino A. Bit†, Jack A. Brown†, Neil R. Carlson‡, Chun-wa Chung†, Anthony W. J. Cooper†, Peter D. Craggs†, Robert P. Davis†, Tony W. Dean†, John P. Eva Source Type: research

[ASAP] Structure –Activity Relationship in Pyrazolo[4,3- < italic toggle="yes" > c < /italic > ]pyridines, First Inhibitors of PEX14 –PEX5 Protein–Protein Interaction with Trypanocidal Activity
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.9b01876 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 6, 2020 Category: Chemistry Authors: Maciej Dawidowski* †‡§, Vishal C. Kalel?, Valeria Napolitano?#, Roberto Fino†‡, Kenji Schorpp¶, Leonidas Emmanouilidis†‡§§, Dominik Lenhart†‡?, Michael Ostertag†‡, Marcel Kaiser??, Marta Kolonko†††, Bettina Tippler?, Wolfgang Source Type: research

[ASAP] Application of Fluorine- and Nitrogen-Walk Approaches: Defining the Structural and Functional Diversity of 2-Phenylindole Class of Cannabinoid 1 Receptor Positive Allosteric Modulators
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.9b01142 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 3, 2020 Category: Chemistry Authors: Sumanta Garai †‡, Pushkar M. Kulkarni†‡, Peter C. Schaffer†, Luciana M. Leo?, Asher L. Brandt?, Ayat Zagzoog?, Tallan Black?, Xiaoyan Lin£, Dow P. Hurst?, David R. Janero§, Mary E. Abood?, Anaelle Zimmowitch£, Alex Straiker£, Roger G. Pertwe Source Type: research

[ASAP] < italic toggle="yes" > In Vivo Veritas < /italic > : < sup > 18 < /sup > F-Radiolabeled Glycomimetics Allow Insights into the Pharmacological Fate of Galectin-3 Inhibitors
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.9b01692 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 3, 2020 Category: Chemistry Authors: Klas Bratteby †‡§?, Edvard Torkelsson‡§, Elina Tampio L’Estrade†‡?, Kristoffer Peterson§, Vladimir Shalgunov†??, Mengfei Xiong†?, Hakon Leffler#, Fredrik R. Zetterberg?, Tomas G. Olsson‡, Nic Gillings?, Ulf J. Nilsson§, Matthias M. H Source Type: research

[ASAP] Correction to Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.9b02072 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 3, 2020 Category: Chemistry Authors: Yu Zou, Di Zhao, Chang Yan, Yanpeng Ji, Jin Liu, Jinyi Xu, Yisheng Lai, Jide Tian, Yihua Zhang*, and Zhangjian Huang* Source Type: research

[ASAP] Potent, Orally Bioavailable, and Efficacious Macrocyclic Inhibitors of Factor XIa. Discovery of Pyridine-Based Macrocycles Possessing Phenylazole Carboxamide P1 Groups
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.9b01768 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 2, 2020 Category: Chemistry Authors: James R. Corte* †, Donald J. P. Pinto*†, Tianan Fang†, Honey Osuna†, Wu Yang†, Yufeng Wang†, Amy Lai†, Charles G. Clark†, Jung-Hui Sun‡, Richard Rampulla‡, Arvind Mathur‡, Mahammed Kaspady§, Premsai Rai Neithnadka§, Yi-Xin Cindy Li Source Type: research

[ASAP] Design of Bimodal Ligands of Neurotensin Receptor 1 for Positron Emission Tomography Imaging and Fluorescence-Guided Surgery of Pancreatic Cancer
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.9b01407 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 2, 2020 Category: Chemistry Authors: Emma Renard †, Pierre-Alix Dancer‡, Christophe Portal§, Franck Denat†, Aure´lie Prignon*?, and Victor Goncalves*† Source Type: research

[ASAP] Discovery and Characterization of 1 < italic toggle="yes" > H < /italic > -1,2,3-Triazole Derivatives as Novel Prostanoid EP4 Receptor Antagonists for Cancer Immunotherapy
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.9b01269 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - January 2, 2020 Category: Chemistry Authors: Jun-Jie Yang †, Wei-Wei Yu†, Long-Long Hu, Wen-Juan Liu, Xian-Hua Lin, Wei Wang, Qiansen Zhang, Pei-Li Wang, Shuo-Wen Tang, Xin Wang, Mingyao Liu, Weiqiang Lu*, and Han-Kun Zhang* Source Type: research

[ASAP] Novel Cell-Penetrating Peptide Conjugated Proteasome Inhibitors: Anticancer and Antifungal Investigations
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.9b01694 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - December 31, 2019 Category: Chemistry Authors: Kamal D. Patel †, Gayan Heruka De Zoysa†, Manju Kanamala‡, Krunal Patel†, Lisa I. Pilkington†, David Barker†, Jo´hannes Reynisson?, Zimei Wu‡, and Vijayalekshmi Sarojini*†§ Source Type: research