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Design and Synthesis of 3-(2H-Chromen-3-yl)-5-aryl-1,2,4-oxadiazole Derivatives as Novel Toll-like Receptor 2/1 Agonists That Inhibit Lung Cancer In Vitro and In Vivo J. Med. Chem. (IF 7.3) Pub Date : 2024-03-18 Yijie Wang, Xu Cheng, Xinru Liu, Jing Xu, Lin Wang, Shouguo Zhang, Shuchen Liu, Tao Peng
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Discovery of Conformationally Constrained ALK2 Inhibitors J. Med. Chem. (IF 7.3) Pub Date : 2024-03-18 Héctor González-Álvarez, Deeba Ensan, Tao Xin, Jong Fu Wong, Carlos A. Zepeda-Velázquez, Julien Cros, Laurent Hoffer, Taira Kiyota, Brian J. Wilson, Ahmed Aman, Owen Roberts, Methvin B. Isaac, Alex N. Bullock, David Smil, Rima Al-awar
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Beyond Rule of Five and PROTACs in Modern Drug Discovery: Polarity Reducers, Chameleonicity, and the Evolving Physicochemical Landscape J. Med. Chem. (IF 7.3) Pub Date : 2024-03-18 Edward Price, Manuel Weinheimer, Alexey Rivkin, Gary Jenkins, Marjoleen Nijsen, Philip B. Cox, David DeGoey
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A Selective-Tumor-Penetrating Strategy via Unidirectional Direct Transfer for Intravesical Therapy of Bladder Cancer J. Med. Chem. (IF 7.3) Pub Date : 2024-03-18 Xiaowen Qin, Heng Wang, Wentao Xu, Bin Zheng, Haibao Zhang, Qi Zhang, Yang Liu, Zhenghong Liu, Li Sun, Yixuan Mou, Cenchao Yao, Wei Zheng, Yiyang Chen, Chenkai Wang, Xuanyi Zhou, Youqing Shen, Pu Zhang, Dahong Zhang
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Identification of Dihydrobenzofuran Neolignans as Novel PDE4 Inhibitors and Evaluation of Antiatopic Dermatitis Efficacy in DNCB-Induced Mice Model J. Med. Chem. (IF 7.3) Pub Date : 2024-03-15 Chenming Gu, Jiayuan Liu, Fei Qian, Wenchao Yu, Doudou Huang, Jingshan Shen, Chenguo Feng, Kaixian Chen, Yiming Li, Xiangrui Jiang, Yechun Xu, Liuqiang Zhang
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Development of Membrane-Targeting Fluorescent 2-Phenyl-1H-phenanthro[9,10-d]imidazole-Antimicrobial Peptide Mimic Conjugates against Methicillin-Resistant Staphylococcus aureus J. Med. Chem. (IF 7.3) Pub Date : 2024-03-16 Ting Xu, Xiaoting Yan, Ayue Kang, Longhua Yang, Xinhui Li, Yue Tian, Ruige Yang, Shangshang Qin, Yong Guo
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Discovery of New Tricyclic Oxime Sampangine Derivatives as Potent Antifungal Agents for the Treatment of Cryptococcosis and Candidiasis J. Med. Chem. (IF 7.3) Pub Date : 2024-03-15 Wanzhen Yang, Ruxiong Liu, Zhuang Li, Jie Tu, Dongjian Xu, Na Liu, Chunquan Sheng
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Cyclic Peptide Keap1–Nrf2 Protein–Protein Interaction Inhibitors: Design, Synthesis, and In Vivo Treatment of Acute Lung Injury J. Med. Chem. (IF 7.3) Pub Date : 2024-03-14 Jihua Zou, Jianyu Yan, Yifei Lu, Zhou Yu, Kai Zhang, Qianyu Han, Dan Han, Conghao Gai, Xiaoyun Chai, Qingjie Zhao, Chunlin Zhuang, Yan Zou
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Covalent Fragment Screening and Optimization Identifies the Chloroacetohydrazide Scaffold as Inhibitors for Ubiquitin C-terminal Hydrolase L1 J. Med. Chem. (IF 7.3) Pub Date : 2024-03-15 Ryan D. Imhoff, Rishi Patel, Muhammad Hassan Safdar, Hannah B. L. Jones, Adan Pinto-Fernandez, Iolanda Vendrell, Hao Chen, Christine S. Muli, Aaron D. Krabill, Benedikt M. Kessler, Michael K. Wendt, Chittaranjan Das, Daniel P. Flaherty
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Identification of a Novel Selective CDK9 Inhibitor for the Treatment of CRC: Design, Synthesis, and Biological Activity Evaluation J. Med. Chem. (IF 7.3) Pub Date : 2024-03-15 Ye Zhong, Jing Xu, Ruochen Zhou, Li Tang, Shaoyue Ding, Zhaohui Ren, Ning Song, Baichun Hu, Huali Yang, Yili Sun, Maosheng Cheng, Jia Li, Yang Liu
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Synthetic Approaches to the New Drugs Approved During 2022 J. Med. Chem. (IF 7.3) Pub Date : 2024-03-15 Scott P. France, Erick A. Lindsey, Emma L. McInturff, Simon Berritt, Daniel W. Carney, Jacob C. DeForest, Sarah J. Fink, Andrew C. Flick, Tony S. Gibson, Kaitlyn Gray, Amber M. Johnson, Carolyn A. Leverett, Yiyang Liu, Subham Mahapatra, Rebecca B. Watson
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Unraveling the Promise of RET Inhibitors in Precision Cancer Therapy by Targeting RET Mutations J. Med. Chem. (IF 7.3) Pub Date : 2024-03-14 Zi-Xuan Wang, Qing-Qing Li, Jiao Cai, Jia-Zhen Wu, Jing-Jing Wang, Meng-Yuan Zhang, Qing-Xin Wang, Zhen-Jiang Tong, Jin Yang, Tian-Hua Wei, Yun Zhou, Wei-Chen Dai, Ning Ding, Xue-Jiao Leng, Shan-Liang Sun, Xin Xue, Yan-Cheng Yu, Ye Yang, Nian-Guang Li, Zhi-Hao Shi
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Subtle Structural Changes across the Boundary between A2AR/A2BR Dual Antagonism and A2BR Antagonism: A Novel Class of 2-Aminopyrimidine-Based Derivatives J. Med. Chem. (IF 7.3) Pub Date : 2024-03-14 Haojie Wang, Xinyu Yang, Yan Li, Shuyin Ze, Bo Feng, Yuan Weng, Aoqi Gao, Gaojie Song, Mingyao Liu, Qiong Xie, Yonghui Wang, Weiqiang Lu
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Arginine-Selective Bioconjugation Reagent for Effective 18F-labeling of Native Proteins J. Med. Chem. (IF 7.3) Pub Date : 2024-03-13 Pragalath Sadasivam, Shivashankar Khanapur, Siddesh V. Hartimath, Boominathan Ramasamy, Peter Cheng, Chin Zan Feng, David Green, Christopher Davis, Julian L. Goggi, Edward G. Robins, Ran Yan
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Discovery of the sEH Inhibitor Epoxykynin as a Potent Kynurenine Pathway Modulator J. Med. Chem. (IF 7.3) Pub Date : 2024-03-12 Lara Dötsch, Caitlin Davies, Elisabeth Hennes, Julia Schönfeld, Adarsh Kumar, Celine Da Cruz Lopes Guita, Johanna H.M. Ehrler, Kerstin Hiesinger, Sasikala Thavam, Petra Janning, Sonja Sievers, Stefan Knapp, Ewgenij Proschak, Slava Ziegler, Herbert Waldmann
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Correction to “Macrocyclic Immunoproteasome Inhibitors as a Potential Therapy for Alzheimer’s Disease” J. Med. Chem. (IF 7.3) Pub Date : 2024-03-12 Min Jae Lee, Deepak Bhattarai, Hyeryung Jang, Ahreum Baek, In Jun Yeo, Seongsoo Lee, Zachary Miller, Sukyeong Lee, Jin Tae Hong, Dong-Eun Kim, Wooin Lee, Kyung Bo Kim
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DNA Interaction and Cleavage Modes of Anthraquinone-Fused Enediynes: A Study on Tiancimycins, Yangpumicins, and Their Semisynthetic Analogues J. Med. Chem. (IF 7.3) Pub Date : 2024-03-14 Zhongqing Wen, Zhoukang Zhuang, Huiming Liu, Zilong Wang, Xueqiong Feng, Xiangcheng Zhu, Xiaohui Yan, Yanwen Duan, Yong Huang
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Discovery of a Novel Thienopyrimidine Compound as a Urate Transporter 1 and Glucose Transporter 9 Dual Inhibitor with Improved Efficacy and Favorable Druggability J. Med. Chem. (IF 7.3) Pub Date : 2024-03-14 Xiaoyu Shi, Tong Zhao, Shuo Wang, Shujing Xu, Hui Liao, Shenghua Gao, Zhen Gao, Jian Zhang, Danhui Qi, Zhijiao Zhang, Fengxin Zheng, Youzhao Wang, Zhenqian Wang, Mingyu Yang, Qian Yang, Fan Yi, Jianxin Pang, Xinyong Liu, Peng Zhan
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Structure-Guided Design and Optimization of Covalent VHL-Targeted Sulfonyl Fluoride PROTACs J. Med. Chem. (IF 7.3) Pub Date : 2024-03-13 Rishi R. Shah, Elena De Vita, Preethi S. Sathyamurthi, Daniel Conole, Xinyue Zhang, Elliot Fellows, Eleanor R. Dickinson, Carlos M. Fleites, Markus A. Queisser, John D. Harling, Edward W. Tate
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Rational Design of PARP1/c-Met Dual Inhibitors for Overcoming PARP1 Inhibitor Resistance Induced by c-Met Overexpression J. Med. Chem. (IF 7.3) Pub Date : 2024-03-13 Zeren Sun, Lanjie Li, Bingxin Zhai, Mengxuan Hu, Lei Huang, Shihui Huang, Liu Ye, Xiangying Kong, Jie Xu, Jie Bai, Jingjie Yan, Qichen Zhou, Zheqi Hu, Yuchen Zhang, Yuhan Jiang, Yan Zhang, Zhou Qiao, Yi Zou, Yungen Xu, Qihua Zhu
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Discovery of Pyridopyrimidinones that Selectively Inhibit the H1047R PI3Kα Mutant Protein J. Med. Chem. (IF 7.3) Pub Date : 2024-03-13 John M. Ketcham, Stephen J. Harwood, Ruth Aranda, Athenea N. Aloiau, Briana M. Bobek, David M. Briere, Aaron C. Burns, Kersti Caddell Haatveit, Andrew Calinisan, Jeffery Clarine, Adam Elliott, Lars D. Engstrom, Robin J. Gunn, Anthony Ivetac, Benjamin Jones, Jon Kuehler, J. David Lawson, Natalie Nguyen, Cody Parker, Kelly E. Pearson, Lisa Rahbaek, Barbara Saechao, Xiaolun Wang, Anna Waters, Laura Waters
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Retro-Inverso Collagen Modulator Peptide Derived from Serpin A1 with Enhanced Stability and Activity In Vitro J. Med. Chem. (IF 7.3) Pub Date : 2024-03-12 Fosca Errante, Marco Pallecchi, Gianluca Bartolucci, Elena Frediani, Francesca Margheri, Lisa Giovannelli, Anna M. Papini, Paolo Rovero
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Discovery of CBPD-268 as an Exceptionally Potent and Orally Efficacious CBP/p300 PROTAC Degrader Capable of Achieving Tumor Regression J. Med. Chem. (IF 7.3) Pub Date : 2024-03-13 Zhixiang Chen, Mi Wang, Dimin Wu, Longchuan Bai, Tianfeng Xu, Hoda Metwally, Yu Wang, Donna McEachern, Lijie Zhao, Ruiting Li, John Takyi-Williams, Meilin Wang, Lu Wang, Qiuxia Li, Bo Wen, Duxin Sun, Shaomeng Wang
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Mechanism-Based Macrocyclic Inhibitors of Serine Proteases J. Med. Chem. (IF 7.3) Pub Date : 2024-03-13 Vishnu C. Damalanka, Victoria Banas, Paolo De Bona, Maithri M. Kashipathy, Kevin Battaile, Scott Lovell, James W. Janetka
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Development of Cytotoxic GW7604-Zeise’s Salt Conjugates as Multitarget Compounds with Selectivity for Estrogen Receptor- Positive Tumor Cells J. Med. Chem. (IF 7.3) Pub Date : 2024-03-13 Patricia Grabher, Paul Kapitza, Nikolas Hörmann, Amelie Scherfler, Martin Hermann, Michael Zwerger, Hristo P. Varbanov, Brigitte Kircher, Daniel Baecker, Ronald Gust
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Synthesis of Sorafenib−Ruthenium Complexes, Investigation of Biological Activities and Applications in Drug Delivery Systems as an Anticancer Agent J. Med. Chem. (IF 7.3) Pub Date : 2024-03-12 Belma Zengin Kurt, Dilek Öztürk Civelek, Elmas Begüm Çakmak, Yakup Kolcuoğlu, Halil Şenol, Begüm Nurpelin Sağlık Özkan, Aydan Dag, Kadriye Benkli
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Searching for Conjugates as New Structures for Antifungal Therapies J. Med. Chem. (IF 7.3) Pub Date : 2024-03-12 Izabela Muszalska-Kolos, Piotr Mariusz Dwiecki
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Discovery and Optimization of Selective Brain-Penetrant EBP Inhibitors that Enhance Oligodendrocyte Formation J. Med. Chem. (IF 7.3) Pub Date : 2024-03-12 Ruth Dorel, Dawei Sun, Nicholas Carruthers, Georgette M. Castanedo, Peter M.-U. Ung, Daniel C. Factor, Tianbo Li, Hannah Baumann, Danielle Janota, Jodie Pang, Laurent Salphati, Robert Meklemburg, Allison J. Korman, Halie E. Harper, Samantha Stubblefield, Jian Payandeh, Daniel McHugh, Bradley T. Lang, Paul J. Tesar, Edward Dere, Matthieu Masureel, Drew J. Adams, Matthew Volgraf, Marie-Gabrielle Braun
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Structure-Guided Elaboration of a Fragment-Like Hit into an Orally Efficacious Leukotriene A4 Hydrolase Inhibitor J. Med. Chem. (IF 7.3) Pub Date : 2024-03-12 Gebhard Thoma, Wolfgang Miltz, Honnappa Srinivas, Carlos A. Penno, Michael Kiffe, Monika Gajewska, Kai Klein, Amanda Evans, Christian Beerli, Till A. Röhn
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Correction to “MicroCycle: An Integrated and Automated Platform to Accelerate Drug Discovery” J. Med. Chem. (IF 7.3) Pub Date : 2024-03-12 Cara E. Brocklehurst, Eva Altmann, Jérôme André, Corentin Bon, Thomas Caya, Holly Davis, Odile Decoret, David Dunstan, Peter Ertl, Carol Ginsburg-Moraff, Jonathan Grob, Daniel J. Gosling, Guillaume Lapointe, Dyuti Majumdar, Alexander N. Marziale, Heinrich Mues, Marco Palmieri, Sophie Racine, Richard I. Robinson, Clayton Springer, Kian Tan, William Ulmer, Laura West, René Wyler
We are adding five authors who were erroneously missing from the original author list. All five contributed significantly to the building, testing, and evaluation of the MicroCycle platform, and their inclusion as authors is well warranted. The five additional authors are Jérôme André, Thomas Caya, Odile Decoret, Dyuti Majumdar, and Laura West. The additions are reflected in the authorship of this
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Development of a Series of Pyrrolopyridone MAT2A Inhibitors J. Med. Chem. (IF 7.3) Pub Date : 2024-03-11 Stephen J. Atkinson, Sharan K. Bagal, Argyrides Argyrou, Sean Askin, Tony Cheung, Elisabetta Chiarparin, Muireann Coen, Iain T. Collie, Ian L. Dale, Claudia De Fusco, Keith Dillman, Laura Evans, Lyman J. Feron, Alison J. Foster, Michael Grondine, Vasudev Kantae, Gillian M. Lamont, Scott Lamont, James T. Lynch, Sten Nilsson Lill, Graeme R. Robb, Jamal Saeh, Marianne Schimpl, James S. Scott, James Smith
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The Discovery of 7-Isopropoxy-2-(1-methyl-2-oxabicyclo[2.1.1]hexan-4-yl)-N-(6-methylpyrazolo[1,5-a]pyrimidin-3-yl)imidazo[1,2-a]pyrimidine-6-carboxamide (BIO-7488), a Potent, Selective, and CNS-Penetrant IRAK4 Inhibitor for the Treatment of Ischemic Stroke J. Med. Chem. (IF 7.3) Pub Date : 2024-03-11 Ryan Evans, Philippe N. Bolduc, Magnus Pfaffenbach, Fang Gao, Tricia May-Dracka, Terry Fang, Brian T. Hopkins, Jayanth V Chodaparambil, Kate L. Henry, Pei Li, Claire Metrick, Ashley Nelson, Patrick Trapa, Ankur Thomas, Linda Burkly, Emily A. Peterson
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Design, Synthesis, and Biological Evaluation of 5-(5-Iodo-2-isopropyl-4-methoxyphenoxy)pyrimidine-2,4-diamine (AF-353) Derivatives as Novel DHFR Inhibitors against Staphylococcus aureus J. Med. Chem. (IF 7.3) Pub Date : 2024-03-11 Zongkai Huang, Xupeng Gou, Xudong Hang, Ting Shi, Jiaxing Yang, Yan Liu, Xinlian He, Jin Li, Keao Quan, Hongkai Bi, Youfu Luo
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Uncovering PROTAC Sensitivity and Efficacy by Multidimensional Proteome Profiling: A Case for STAT3 J. Med. Chem. (IF 7.3) Pub Date : 2024-03-11 Yuying Suo, Daohai Du, Chao Chen, Hongwen Zhu, Xiongjun Wang, Nixue Song, Dayun Lu, Yaxi Yang, Jiacheng Li, Jun Wang, Zhongyuan Luo, Bing Zhou, Cheng Luo, Hu Zhou
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Engineering of a Biologically Active Glycosylated Glucagon-Like Peptide-1 Analogue J. Med. Chem. (IF 7.3) Pub Date : 2024-03-11 Chaitra Chandrashekar, Feng Lin, Yuji Nishiuchi, Sam F. Mohammed, Barbara F. White, Yanni Arsenakis, Elita Yuliantie, Peishen Zhao, Sam van Dun, Anna Koijen, Yasuhiro Kajihara, Denise Wootten, Garron T. Dodd, Leendert J. van den Bos, John D. Wade, Mohammed Akhter Hossain
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Discovery of Novel PD-L1 Small-Molecular Inhibitors with Potent In Vivo Anti-tumor Immune Activity J. Med. Chem. (IF 7.3) Pub Date : 2024-03-11 Liu Liu, Honghan Zhang, Jie Hou, Yuying Zhang, Luosen Wang, Shijun Wang, Zhiying Yao, Tao Xie, Xiaoan Wen, Qinglong Xu, Liang Dai, Zhiqi Feng, Pu Zhang, Yaojun Wu, Hongbin Sun, Jun Liu, Haoliang Yuan
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Fragment-Based Discovery of Allosteric Inhibitors of SH2 Domain-Containing Protein Tyrosine Phosphatase-2 (SHP2) J. Med. Chem. (IF 7.3) Pub Date : 2024-03-10 James E. H. Day, Valerio Berdini, Joan Castro, Gianni Chessari, Thomas G. Davies, Philip J. Day, Jeffrey D. St. Denis, Hideto Fujiwara, Satoshi Fukaya, Christopher C. F. Hamlett, Keisha Hearn, Steven D. Hiscock, Rhian S. Holvey, Satoru Ito, Navrohit Kandola, Yasuo Kodama, John W. Liebeschuetz, Vanessa Martins, Kenichi Matsuo, Paul N. Mortenson, Sandra Muench, Yoko Nakatsuru, Hiroaki Ochiiwa, Nicholas
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Photochemistry in Medicinal Chemistry and Chemical Biology J. Med. Chem. (IF 7.3) Pub Date : 2024-03-08 W. Felix Zhu, Claire Empel, Sveva Pelliccia, Rene M. Koenigs, Ewgenij Proschak, Victor Hernandez-Olmos
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A Robust Platform for the Molecular Design of Potent, Protease-Stable, Long-Acting GIP Analogues J. Med. Chem. (IF 7.3) Pub Date : 2024-03-08 Kathleen M. Sicinski, Damla Sürmeli, Jasper Du, Venkata S. Raman, Vittorio Montanari, Minhee Lee, Benjamin N. Harwood, Alan S. Kopin, Martin Beinborn, Krishna Kumar
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Design, Synthesis, and Structure–Activity Relationship of Novel Pyridazinone-Based PARP7/HDACs Dual Inhibitors for Elucidating the Relationship between Antitumor Immunity and HDACs Inhibition J. Med. Chem. (IF 7.3) Pub Date : 2024-03-08 Ji-Long Duan, Chen-Chen Wang, Yinghui Yuan, Zi Hui, Hang Zhang, Nian-Dong Mao, Pengpeng Zhang, Bowen Sun, Jing Lin, Zishuo Zhang, Yuan Gao, Tian Xie, Xiang-Yang Ye
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Empowering Voices: Inspiring Women in Medicinal Chemistry J. Med. Chem. (IF 7.3) Pub Date : 2024-03-08 Maria-Jesus Blanco, Joanne J. Bronson, Erin F. DiMauro, Carolyn Dzierba, MariJean Eggen, Amanda L. Garner, Gunda Georg, Jeanine Giarolla, Nicole C. Goodwin, Melissa C. Grenier-Davies, Carrie Haskell-Luevano, Ulrike Holzgrabe, Rong Huang, H. Rachel Lagiakos, Katerina Leftheris, Yvonne Martin, Maria João Matos, Tricia L. May-Dracka, Christa E. Müller, Amy H. Newman, Emma Parmee, Jennifer C. Petter, Nuria
As we celebrate International Women’s Day 2024 with the theme “Inspire Inclusion”, the women of the ACS Medicinal Chemistry Division (MEDI) want to foster a sense of belonging, relevance, and empowerment by sharing uplifting stories of what inspired them to become medicinal chemists. In this editorial, we are featuring female medicinal chemistry scientists to provide role models, encouragement, and
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Structure–Activity Relationships of Natural and Semisynthetic Plecomacrolides Suggest Distinct Pathways for HIV-1 Immune Evasion and Vacuolar ATPase-Dependent Lysosomal Acidification J. Med. Chem. (IF 7.3) Pub Date : 2024-03-07 Morgan McCauley, Matthew Huston, Alanna R. Condren, Filipa Pereira, Joel Cline, Marianne Yaple-Maresh, Mark M. Painter, Gretchen E. Zimmerman, Andrew W. Robertson, Nolan Carney, Christopher Goodall, Valeri Terry, Rolf Müller, David H. Sherman, Kathleen L. Collins
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Cardiac Troponin Activator CK-963 Increases Cardiac Contractility in Rats J. Med. Chem. (IF 7.3) Pub Date : 2024-03-07 Scott E. Collibee, Antonio Romero, Alexander R. Muci, Darren T. Hwee, Chihyuan Chuang, James J. Hartman, Alykhan S. Motani, Luke Ashcraft, Andre DeRosier, Mark Grillo, Qing Lu, Fady I. Malik, Bradley P. Morgan
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Novel Re(I) Complexes as Potential Selective Theranostic Agents in Cancer Cells and In Vivo in Caenorhabditis elegans Tumoral Strains J. Med. Chem. (IF 7.3) Pub Date : 2024-03-07 Alicia Marco, Pezhman Ashoo, Samanta Hernández-García, Pedro Martínez-Rodríguez, Natalia Cutillas, Annette Vollrath, Dustin Jordan, Christoph Janiak, Fernando Gandía-Herrero, José Ruiz
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Theranostic Agent Targeting Bone Metastasis: A Novel [68Ga]Ga/[177Lu]Lu-DOTA-HBED-bisphosphonate J. Med. Chem. (IF 7.3) Pub Date : 2024-03-07 Wenbin Jin, Ruiyue Zhao, Ran Wang, Seok Rye Choi, Karl Ploessl, David Alexoff, Zehui Wu, Lin Zhu, Hank F. Kung
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Lipophilic Group-Modified Manganese(II)-Based Contrast Agents for Vascular and Hepatobiliary Magnetic Resonance Imaging J. Med. Chem. (IF 7.3) Pub Date : 2024-03-07 Zhongyuan Cai, Lingling Jiang, Yingzi Cao, Shengxiang Fu, Shasha Wang, Yuting Jiang, Haojie Gu, Na Li, Xiaomin Fu, Shimin Tang, Jiang Zhu, Weidong Cao, Lei Zhong, Zhuzhong Cheng, Chunchao Xia, Su Lui, Bin Song, Qiyong Gong, Hua Ai
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Novel β-Hairpin Antimicrobial Peptide Containing the β-Turn Sequence of -NG- and the Tryptophan Zippers Facilitate Self-Assembly into Nanofibers, Exhibiting Excellent Antimicrobial Performance J. Med. Chem. (IF 7.3) Pub Date : 2024-03-04 Beibei Li, Xu Ouyang, Yao Liu, Zufang Ba, Yinyin Yang, Jingying Zhang, Ping Yang, Tingting Yang, Yu Wang, Yuhuan Zhao, Wenbo Mao, Chao Zhong, Hui Liu, Yun Zhang, Sanhu Gou, Jingman Ni
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The Molecular Theory of Sweet Taste: Revisit, Update, and Beyond J. Med. Chem. (IF 7.3) Pub Date : 2024-03-05 Hong Zheng, Xiangqun Xu, Yishan Fang, Rui Sun, Bo Liu
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A Vancomycin-Templated DNA-Encoded Library for Combating Drug-Resistant Bacteria J. Med. Chem. (IF 7.3) Pub Date : 2024-03-05 Dongliang Guan, Jiaxiang Liu, Feifei Chen, Jian Li, Xiaowen Wang, Weiwei Lu, Yanrui Suo, Feng Tang, Lefu Lan, Xiaojie Lu, Wei Huang
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Designing a Mitochondria-Targeted Theranostic Cyclometalated Iridium(III) Complex: Overcoming Cisplatin Resistance and Inhibiting Tumor Metastasis through Necroptosis and Immune Response J. Med. Chem. (IF 7.3) Pub Date : 2024-03-05 Wenjuan Li, Ting Li, Ying Pan, Shanhe Li, Gang Xu, Zhenlei Zhang, Hong Liang, Feng Yang
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Development and In Vivo Evaluation of Small-Molecule Ligands for Positron Emission Tomography of Immune Checkpoint Modulation Targeting Programmed Cell Death 1 Ligand 1 J. Med. Chem. (IF 7.3) Pub Date : 2024-03-05 Karsten Bamminger, Verena Pichler, Chrysoula Vraka, Tanja Limberger, Boryana Moneva, Katharina Pallitsch, Barbara Lieder, Anna Sophia Zacher, Stefanie Ponti, Katarína Benčurová, Jiaye Yang, Sandra Högler, Petra Kodajova, Lukas Kenner, Marcus Hacker, Wolfgang Wadsak
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Discovery of RORγ Allosteric Fluorescent Probes and Their Application: Fluorescence Polarization, Screening, and Bioimaging J. Med. Chem. (IF 7.3) Pub Date : 2024-03-05 Yan-Cheng Yu, Zhen-Jiang Tong, Xiao-Ting Liang, Jia-Zhen Wu, Yu-Jing Xu, Jing-Jing Wang, Meng-Yuan Zhang, Tian-Hua Wei, Jin Yang, Yi-Bo Wang, Qing-Xin Wang, Qing-Qing Li, Zixuan Wang, XueJiao Leng, Ning Ding, Xin Xue, Shan-Liang Sun, Nian-Guang Li, Xiao-Long Wang
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Discovery and Characterization of a New Class of C5aR1 Antagonists Showing In Vivo Activity J. Med. Chem. (IF 7.3) Pub Date : 2024-03-04 Francis Hubler, Dorte Renneberg, Hervé Siendt, Simon Stamm, Kurt Hilpert, Eva Caroff, Stephane Delahaye, Sylvie Froidevaux, Mark J. Murphy
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Dual Inhibitors of Brain Carbonic Anhydrases and Monoamine Oxidase-B Efficiently Protect against Amyloid-β-Induced Neuronal Toxicity, Oxidative Stress, and Mitochondrial Dysfunction J. Med. Chem. (IF 7.3) Pub Date : 2024-03-04 Simone Giovannuzzi, Daniel Chavarria, Gustavo Provensi, Manuela Leri, Monica Bucciantini, Simone Carradori, Alessandro Bonardi, Paola Gratteri, Fernanda Borges, Alessio Nocentini, Claudiu T. Supuran
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Discovery of TRPA1 Antagonist GDC-6599: Derisking Preclinical Toxicity and Aldehyde Oxidase Metabolism with a Potential First-in-Class Therapy for Respiratory Disease J. Med. Chem. (IF 7.3) Pub Date : 2024-03-03 Jack A. Terrett, Justin Q. Ly, Paula Katavolos, Catrin Hasselgren, Steven Laing, Fiona Zhong, Elisia Villemure, Martin Déry, Robin Larouche-Gauthier, Huifen Chen, Daniel G. Shore, Wyne P. Lee, Eric Suto, Kevin Johnson, Marjory Brooks, Alyssa Stablein, Francis Beaumier, Léa Constantineau-Forget, Chantal Grand-Maître, Luce Lépissier, Stéphane Ciblat, Claudio Sturino, Yong Chen, Baihua Hu, Justin Elstrott
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A Novel NMR-Based Protocol to Screen Ultralow Molecular Weight Fragments J. Med. Chem. (IF 7.3) Pub Date : 2024-03-01 Annagiulia Favaro, Mattia Sturlese
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Structural Basis for Molecular Recognition of Cannabinoids by Inhibitory Cys-Loop Channels J. Med. Chem. (IF 7.3) Pub Date : 2024-03-01 Lautaro D. Alvarez, N. R. Carina Alves
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Structure-Based Discovery of High-Affinity Small Molecule Ligands and Development of Tool Probes to Study the Role of Chitinase-3-Like Protein 1 J. Med. Chem. (IF 7.3) Pub Date : 2024-03-01 Wojciech Czestkowski, Łukasz Krzemiński, Michał C. Piotrowicz, Marzena Mazur, Elżbieta Pluta, Gleb Andryianau, Robert Koralewski, Krzysztof Matyszewski, Sylwia Olejniczak, Michał Kowalski, Katarzyna Lisiecka, Rafał Kozieł, Katarzyna Piwowar, Diana Papiernik, Marcin Nowotny, Agnieszka Napiórkowska-Gromadzka, Elżbieta Nowak, Dorota Niedziałek, Grzegorz Wieczorek, Anna Siwińska, Tomasz Rejczak, Karol
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Development of Selective Pyrido[2,3-d]pyrimidin-7(8H)-one-Based Mammalian STE20-Like (MST3/4) Kinase Inhibitors J. Med. Chem. (IF 7.3) Pub Date : 2024-02-29 Marcel Rak, Amelie Menge, Roberta Tesch, Lena M. Berger, Dimitrios-Ilias Balourdas, Ekaterina Shevchenko, Andreas Krämer, Lewis Elson, Benedict-Tilman Berger, Ismahan Abdi, Laurenz M. Wahl, Antti Poso, Astrid Kaiser, Thomas Hanke, Thales Kronenberger, Andreas C. Joerger, Susanne Müller, Stefan Knapp
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Unleashing the Potential of Camptothecin: Exploring Innovative Strategies for Structural Modification and Therapeutic Advancements J. Med. Chem. (IF 7.3) Pub Date : 2024-02-29 Zheng Chen, Maoyu Liu, Ningyu Wang, Wenjing Xiao, Jianyou Shi