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Discovery of A-910, a Highly Potent and Orally Bioavailable Dual MerTK/Axl-Selective Tyrosine Kinase Inhibitor J. Med. Chem. (IF 6.8) Pub Date : 2024-09-16 Yiyun Yu, Miyeon Jang, Julie Miyashiro, Richard F. Clark, Gui-Dong Zhu, Jane Gong, Yujia Dai, Robin R. Frey, Thomas D. Penning, Hadong Kim, Hyung Ki Lee, Jin Kwan Kim, Ki Moon Ryu, Seong Jin Park, Taeyoung Yoon, Tao Li, Matthew D. Kurnick, Nicolas J. Kapecki, Leiming Li, Jacob V. Gorman, Debra A. Montgomery, Vlasios Manaves, Kenneth D. Bromberg, Stella Z. Doktor, Ashish Thakur, Jin Wang, Heath A. Smith
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Enhanced Recognition Memory through Dual Modulation of Brain Carbonic Anhydrases and Cholinesterases J. Med. Chem. (IF 6.8) Pub Date : 2024-09-16 Alessio Nocentini, Alessia Costa, Alessandro Bonardi, Andrea Ammara, Simone Giovannuzzi, Andrea Petreni, Gianluca Bartolucci, Barbara Rani, Manuela Leri, Monica Bucciantini, José G. Fernández-Bolaños, Óscar López, Maria Beatrice Passani, Gustavo Provensi, Paola Gratteri, Claudiu T. Supuran
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Discovery and In Vivo Exploration of 1,3,4-Oxadiazole and α-Fluoroacrylate Containing IL-17 Inhibitors J. Med. Chem. (IF 6.8) Pub Date : 2024-09-14 Juraj Velcicky, Matthias R. Bauer, Achim Schlapbach, Guillaume Lapointe, Arndt Meyer, Markus Vögtle, Ernst Blum, Estelle Ngo, Catherine Rolando, Pierre Nimsgern, Sylvie Teixeira-Fouchard, Hansjoerg Lehmann, Pascal Furet, Frédéric Berst, Jens Schümann, Rowan Stringer, Patrice Larger, Cindy Schmid, Catriona T. Prendergast, Simone Riek, Patrick Schmutz, Sylvie Lehmann, Jörg Berghausen, Clemens Scheufler
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Development of Novel Indole-Based Covalent Inhibitors of TEAD as Potential Antiliver Cancer Agents J. Med. Chem. (IF 6.8) Pub Date : 2024-09-13 Chen Zhou, Chunbao Sun, Wei Zhou, Tian Tian, Daniel C. Schultz, Tong Wu, Mu Yu, Lizi Wu, Liya Pi, Chenglong Li
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Between Theory and Practice: Computational/Experimental Integrated Approaches to Understand the Solubility and Lipophilicity of PROTACs J. Med. Chem. (IF 6.8) Pub Date : 2024-09-13 Andrea Venturi, Stefano Di Bona, Jenny Desantis, Michela Eleuteri, Matteo Bartalucci, Massimo Baroni, Paolo Benedetti, Laura Goracci, Gabriele Cruciani
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Discovery and Development of Highly Potent and Orally Bioavailable Nonpeptidic αvβ6 Integrin Inhibitors J. Med. Chem. (IF 6.8) Pub Date : 2024-09-13 Panayiotis A. Procopiou, John Barrett, Matthew H. J. Crawford, Richard J. D. Hatley, Ashley P. Hancock, John M. Pritchard, James E. Rowedder, Royston C. B. Copley, Robert J. Slack, Steven L. Sollis, Lee R. Thorp, Rhys A. Lippa, Simon J. F. Macdonald, Tim N. Barrett
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Design, Synthesis, and Bioevaluation of Novel NLRP3 Inhibitor with IBD Immunotherapy from the Virtual Screen J. Med. Chem. (IF 6.8) Pub Date : 2024-09-13 Ziwen Zhang, Hongyu Wu, Kai Yin, Xinru Zheng, Zhonglian Cao, Wei Guo, Chunchang Zhao, Xianfeng Gu
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Targeting Thyroid-Stimulating Hormone Receptor: A Perspective on Small-Molecule Modulators and Their Therapeutic Potential J. Med. Chem. (IF 6.8) Pub Date : 2024-09-13 Yu Zhang, Ye Tan, Zian Zhang, Xi Cheng, Jia Duan, Yi Li
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Discovery of SIRT1-Activating Hydrogen Sulfide Donating Derivatives for Efficient Resistant of Myocardial Ischemic Injury J. Med. Chem. (IF 6.8) Pub Date : 2024-09-13 Shenglin Wang, Dongyan Feng, Weirenbo Wang, Chao Zheng, Chaowei Liang, Siqing Li, Haonan Li, Fanxing Xu, Hao Cao, Huiming Hua, Maosheng Cheng, Dahong Li
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Antibacterial and Anti-Inflammatory Activity of Branched Peptides Derived from Natural Host Defense Sequences J. Med. Chem. (IF 6.8) Pub Date : 2024-09-11 Giada Meogrossi, Eva Tollapi, Alessandro Rencinai, Jlenia Brunetti, Silvia Scali, Eugenio Paccagnini, Mariangela Gentile, Pietro Lupetti, Simona Pollini, Gian Maria Rossolini, Andrea Bernini, Alessandro Pini, Luisa Bracci, Chiara Falciani
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CETZOLE Analogs as Potent Ferroptosis Inducers and Their Target Identification Using Covalent/Affinity Probes J. Med. Chem. (IF 6.8) Pub Date : 2024-09-12 Samkeliso Dlamini, Shahrzad Mohajeri, Nishanth Kuganesan, Shaimaa H. Sindi, Endri Karaj, Dewmi S. Rathnayake, Jade McDaniel, William R. Taylor, L. M. Viranga Tillekeratne
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Discovery of 2-Aryl-4-aminoquinazolin-Based LSD1 Inhibitors to Activate Immune Response in Gastric Cancer J. Med. Chem. (IF 6.8) Pub Date : 2024-09-12 Bo Wang, Shu-Wu Wang, Ying Zhou, Shao-Peng Wang, Ya Gao, Hui-Min Liu, Shi-Kun Ji, Sai-Qi Wang, Yi-Chao Zheng, Cheng Zhang, Adil Mardinoglu, Hong-Min Liu, Xiao-Bing Chen, Xing-Jie Dai
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Evaluation of Efficiency of Liposome-Entrapped Iridium(III) Complexes Inhibiting Tumor Growth In Vitro and In Vivo J. Med. Chem. (IF 6.8) Pub Date : 2024-09-12 Huiyan Hu, Jing Chen, Fan Zhang, Zhujun Sheng, Yan Yang, Yufeng Xie, Lin Zhou, Yunjun Liu
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Development of a First-in-Class DNMT1/HDAC Inhibitor with Improved Therapeutic Potential and Potentiated Antitumor Immunity J. Med. Chem. (IF 6.8) Pub Date : 2024-09-12 Yingjie Chang, Huahui Guo, Xue Li, Liangyi Zong, Jiale Wei, Zhihai Li, Cheng Luo, Xinying Yang, Hao Fang, Xiangqian Kong, Xuben Hou
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Tuning RXR Modulators for PGC1α Recruitment J. Med. Chem. (IF 6.8) Pub Date : 2024-09-11 Felix Nawa, Minh Sai, Jan Vietor, Roman Schwarzenbach, Anesa Bitić, Sina Wolff, Niklas Ildefeld, Jörg Pabel, Thomas Wein, Julian A. Marschner, Jan Heering, Daniel Merk
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Inhibition of the EphA2-Sam/Ship2-Sam Association through Peptide Ligands: Studying the Combined Effect of Charge and Aromatic Character J. Med. Chem. (IF 6.8) Pub Date : 2024-09-11 Marian Vincenzi, Flavia A. Mercurio, Rosanna Palumbo, Sara La Manna, Luciano Pirone, Daniela Marasco, Emilia M. Pedone, Marilisa Leone
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Dually Labeled Neurotensin NTS1R Ligands for Probing Radiochemical and Fluorescence-Based Binding Assays J. Med. Chem. (IF 6.8) Pub Date : 2024-09-11 Fabian J. Ertl, Sergei Kopanchuk, Nicola C. Dijon, Santa Veikšina, Maris-Johanna Tahk, Tõnis Laasfeld, Franziska Schettler, Albert O. Gattor, Harald Hübner, Nataliya Archipowa, Johannes Köckenberger, Markus R. Heinrich, Peter Gmeiner, Roger J. Kutta, Nicholas D. Holliday, Ago Rinken, Max Keller
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Targeting HSP90 for Cancer Therapy: Current Progress and Emerging Prospects J. Med. Chem. (IF 6.8) Pub Date : 2024-09-10 Xinqi Liang, Ruixian Chen, Chengdi Wang, Yuxi Wang, Jifa Zhang
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Discovery of SILA-123 as a Highly Potent FLT3 Inhibitor for the Treatment of Acute Myeloid Leukemia with Various FLT3 Mutations J. Med. Chem. (IF 6.8) Pub Date : 2024-09-11 Tian-Hua Wei, Zi-Xuan Wang, Meng-Yi Lu, Yu-Jing Xu, Jin Yang, Xing-Feng Ni, Yang Cheng, Meng-Yuan Zhang, Jia-Chuan Liu, Qing-Qing Li, Jiao Cai, Zi-Jun Chen, Ji-Bo Kang, Nan Li, Wei-Chen Dai, Ning Ding, Yan-Cheng Yu, Xue-Jiao Leng, Xin Xue, Xiao-Long Wang, Shan-Liang Sun, Ye Yang, Nian-Guang Li, Zhi-Hao Shi
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Preclinical Evaluation of Dihydropyrazole-Cored Positron Emission Tomography (PET) Ligands for Imaging of Receptor-Interacting Serine/Threonine Protein Kinase 1 (RIPK1) in the Brain J. Med. Chem. (IF 6.8) Pub Date : 2024-09-11 Wanqing Li, Xiaojun Zhang, Jie Ma, Jingyin Zhou, Xuan Di, Donglan Huang, Kaixiang Zhou, Jinming Zhang, Lu Wang, Hualong Fu, Mengchao Cui
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Discovery of TYRA-300: First Oral Selective FGFR3 Inhibitor for the Treatment of Urothelial Cancers and Achondroplasia J. Med. Chem. (IF 6.8) Pub Date : 2024-09-11 Robert L. Hudkins, Eric Allen, Alexandra Balcer, Isaac D. Hoffman, Samhita Iyer, Melissa Neal, Kirk J. Nelson, Marc Rideout, Qing Ye, Jacqueline H. Starrett, Piyush Patel, Todd Harris, Ronald V. Swanson, Daniel C. Bensen
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Discovery of N-Aryl-N′-[4-(aryloxy)cyclohexyl]squaramide-Based Inhibitors of LXR/SREBP-1c Signaling Pathway Ameliorating Steatotic Liver Disease: Navigating the Role of SIRT6 Activation J. Med. Chem. (IF 6.8) Pub Date : 2024-09-11 Long Huu Nguyen, Ye Eun Cho, Soyeong Kim, Yeonsoo Kim, Jinsook Kwak, Jung-Soo Suh, Jinyoung Lee, Kyuwon Son, Minseong Kim, Eun Seo Jang, Naghyun Song, BuChul Choi, Jiah Kim, Yealin Tak, Taeyeon Hwang, Jeyun Jo, Eun-Woo Lee, Sang-Bum Kim, Sanghyun Kim, Oh-Bin Kwon, Sangok Kim, Seoung Rak Lee, Haeseung Lee, Tae-Jin Kim, Seonghwan Hwang, Hwayoung Yun
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Membrane-Targeting Amphiphilic Honokiol Derivatives Containing an Oxazole Moiety as Potential Antibacterials against Methicillin-Resistant Staphylococcus aureus J. Med. Chem. (IF 6.8) Pub Date : 2024-09-11 Ruige Yang, Liping Cui, Shengnan Xu, Yan Zhong, Ting Xu, Jifeng Liu, Zhenwei Lan, Shangshang Qin, Yong Guo
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Contilisant+Tubastatin A Hybrids: Polyfunctionalized Indole Derivatives as New HDAC Inhibitor-Based Multitarget Small Molecules with In Vitro and In Vivo Activity in Neurodegenerative Diseases J. Med. Chem. (IF 6.8) Pub Date : 2024-09-10 Mireia Toledano-Pinedo, Alicia Porro-Pérez, Linda Schäker-Hübner, Fernando Romero, Min Dong, Abdelouahid Samadi, Pedro Almendros, Isabel Iriepa, Òscar M. Bautista-Aguilera, M. Mercedes Rodríguez-Fernández, Cristina Solana-Manrique, Inmaculada Sanchis, Alba Mora-Morell, Ania Canseco Rodrìguez, Ana M Sànchez-Pérez, Damijan Knez, Stanislav Gobec, Aina Bellver-Sanchis, Belén Pérez, Alexey V. Dobrydnev
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Discovery of Novel Non-nucleoside DOT1LR231Q Inhibitors with Improved Pharmacokinetic Properties and Anti-lung Cancer Efficacy J. Med. Chem. (IF 6.8) Pub Date : 2024-09-10 Zehui Tan, Ning Guo, Shuyu Liu, Jiandong Li, Yu Chen, Jianming Cui, Hongrui Lei, Nan Jiang, Lihui Wang, Xin Zhai
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Structure–Activity Relationship of Inositol Thiophosphate Analogs as Allosteric Activators of Clostridioides difficile Toxin B J. Med. Chem. (IF 6.8) Pub Date : 2024-09-10 Rebecca Cummer, Félix Grosjean, Raphaël Bolteau, Seyed Ehsan Vasegh, Simon Veyron, Liam Keogh, Jean-François Trempe, Bastien Castagner
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Influence of Trp-Cage on the Function and Stability of GLP-1R Agonist Exenatide Derivatives J. Med. Chem. (IF 6.8) Pub Date : 2024-09-10 Dániel Horváth, Pál Stráner, Nóra Taricska, Zsolt Fazekas, Dóra K. Menyhárd, András Perczel
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Identifying Artifacts from Large Library Docking J. Med. Chem. (IF 6.8) Pub Date : 2024-09-10 Yujin Wu, Fangyu Liu, Isabella Glenn, Karla Fonseca-Valencia, Lu Paris, Yuyue Xiong, Steven V. Jerome, Charles L. Brooks, III, Brian K. Shoichet
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Can Machine Learning Overcome the 95% Failure Rate and Reality that Only 30% of Approved Cancer Drugs Meaningfully Extend Patient Survival? J. Med. Chem. (IF 6.8) Pub Date : 2024-09-10 Duxin Sun, Christian Macedonia, Zhigang Chen, Sriram Chandrasekaran, Kayvan Najarian, Simon Zhou, Tim Cernak, Vicki L. Ellingrod, H. V. Jagadish, Bernard Marini, Manjunath Pai, Angela Violi, Jason C. Rech, Shaomeng Wang, Yan Li, Brian Athey, Gilbert S. Omenn
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A Lysosome-Targeting hNEU1 Inhibitor Treats Myocardial Infarction: A Potential Therapeutic Breakthrough J. Med. Chem. (IF 6.8) Pub Date : 2024-09-10 Wen Zhou, Wanxiang Yang, Ping Jiang, Shaohua Gou
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Structure, Function, and Activity of Small Molecule and Peptide Inhibitors of Protein Arginine Methyltransferase 1 J. Med. Chem. (IF 6.8) Pub Date : 2024-09-09 Thordur Hendrickson-Rebizant, Sadhana R. N. Sudhakar, Michael J. Rowley, Adam Frankel, James R. Davie, Ted M. Lakowski
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The “Doorstop Pocket” In Thioredoxin Reductases─An Unexpected Druggable Regulator of the Catalytic Machinery J. Med. Chem. (IF 6.8) Pub Date : 2024-09-09 Matteo Ardini, Sammy Y. Aboagye, Valentina Z. Petukhova, Irida Kastrati, Rodolfo Ippoliti, Gregory R. J. Thatcher, Pavel A. Petukhov, David L. Williams, Francesco Angelucci
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Photoinduction of Ferroptosis and cGAS-STING Activation by a H2S-Responsive Iridium(III) Complex for Cancer-Specific Therapy J. Med. Chem. (IF 6.8) Pub Date : 2024-09-09 Yi Li, Ben Liu, Yue Zheng, Meng Hu, Liu-Yi Liu, Cai-Rong Li, Wei Zhang, Yu-Xiao Lai, Zong-Wan Mao
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Discovery of Thiophene Derivatives as Potent, Orally Bioavailable, and Blood–Brain Barrier-Permeable Ebola Virus Entry Inhibitors J. Med. Chem. (IF 6.8) Pub Date : 2024-09-09 Marcos Morales-Tenorio, Fátima Lasala, Alfonso Garcia-Rubia, Elnaz Aledavood, Michelle Heung, Catherine Olal, Beatriz Escudero-Pérez, Covadonga Alonso, Ana Martínez, César Muñoz-Fontela, Rafael Delgado, Carmen Gil
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Merging Natural Product Structures with Pharmaceutical Leads: Unnatural Enantiomers of Estranes as Glucocorticoid Receptor Modulators That Suppress TNF-α and IL-6 Release J. Med. Chem. (IF 6.8) Pub Date : 2024-09-06 Joshua M. Nicholson, Dexi Yang, Thomas Koelblen, Eric L. Hu, Christopher C. Coss, Thomas P. Burris, Xiao Hu, Glenn C. Micalizio
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A Photoactivatable Version of Ivabradine Enables Light-Induced Block of HCN Current In Vivo J. Med. Chem. (IF 6.8) Pub Date : 2024-09-05 Alessandro Porro, Edoardo Armano, Federico Brandalise, Rebecca Appiani, Monica Beltrame, Andrea Saponaro, Clelia Dallanoce, Koichi Nakajo, Kaei Ryu, Roberta Leone, Gerhard Thiel, Marco Pallavicini, Anna Moroni, Cristiano Bolchi
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Developing a Palladium(II) Agent to Overcome Multidrug Resistance and Metastasis of Liver Tumor by Targeted Multiacting on Tumor Cell, Inactivating Cancer-Associated Fibroblast and Activating Immune Response J. Med. Chem. (IF 6.8) Pub Date : 2024-09-05 Ming Jiang, Wenjuan Li, Jinzhe Liang, Min Pang, Shanhe Li, Gang Xu, Minghui Zhu, Hong Liang, Zhenlei Zhang, Feng Yang
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Development of Tailless Homologue Receptor (TLX) Agonist Chemical Tools J. Med. Chem. (IF 6.8) Pub Date : 2024-09-05 Emily C. Hank, Minh Sai, Till Kasch, Isabelle Meijer, Julian A. Marschner, Daniel Merk
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Structure Tailoring of Hemicyanine Dyes for In Vivo Shortwave Infrared Imaging J. Med. Chem. (IF 6.8) Pub Date : 2024-09-05 Jiaming Guo, Yiling Zhu, Yuqian Qu, Longfei Zhang, Mingxi Fang, Zihan Xu, Tianbao Wang, Yufei Qin, Yihan Xu, Yuying Li, Yimin Chen, Hualong Fu, Xiayu Liu, Yajun Liu, Cheng Liu, Yuan Gao, Mengchao Cui, Kaixiang Zhou
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Antimicrobial Resistance: An Ultimate Challenge for 21st Century Scientists, Healthcare Professionals, and Policymakers to Save Future Generations J. Med. Chem. (IF 6.8) Pub Date : 2024-09-05 Vazahyil Hari Krishnaprasad, Sanjay Kumar
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Tricyclic Benzo[1,3]oxazinyloxazolidinones as Potent Antibacterial Agents against Drug-Resistant Pathogens J. Med. Chem. (IF 6.8) Pub Date : 2024-09-05 Haijia Lu, Xiaowan Han, Di Qin, Li Sheng, Chen Du, Bin Wang, Hongyi Zhao, Yu Lu, Yishuang Liu, Hai-Yu Hu, Ya Liu, Dongfeng Zhang
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Discovery and Evaluation of TLR-Targeted Immune Agonists J. Med. Chem. (IF 6.8) Pub Date : 2024-09-05 Natalia Chernyak, Bhagyashree Bhagwat, Saraswathi Naravula, Ying Chen, Nicolas Solban, Fan Zhang, Esther Kofman, Fahimeh Raoufi, Xibei Dang, Jianming Bao, Daniela Tomazela, Marc Baily, Bernhard Geierstanger, John A. Flygare, Jin-Hwan Han, Aarron Willingham, W. Michael Seganish
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Transferrin-Modified Carprofen Platinum(IV) Nanoparticles as Antimetastasis Agents with Tumor Targeting, Inflammation Inhibition, Epithelial–Mesenchymal Transition Suppression, and Immune Activation Properties J. Med. Chem. (IF 6.8) Pub Date : 2024-09-05 Ming Zhang, Yan Chen, Shuaiqi Feng, Yanqin He, Zhifang Liu, Ning Zhang, Qingpeng Wang
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Structure Activity of β-Amidomethyl Vinyl Sulfones as Covalent Inhibitors of Chikungunya nsP2 Cysteine Protease with Antialphavirus Activity J. Med. Chem. (IF 6.8) Pub Date : 2024-09-05 Anirban Ghoshal, Kesatebrhan Haile Asressu, Mohammad Anwar Hossain, Peter J. Brown, Meganathan Nandakumar, Anand Vala, Eric M. Merten, John D. Sears, Isabella Law, Jane E. Burdick, Noah L. Morales, Sumera Perveen, Kenneth H. Pearce, Konstantin I. Popov, Nathaniel J. Moorman, Mark T. Heise, Timothy M. Willson
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Photostable Iridium(III) Cyclometallated Complex is an Efficient Photosensitizer for Killing Multiple Cancer Cell Lines and 3D Models under Low Doses of Visible Light J. Med. Chem. (IF 6.8) Pub Date : 2024-09-04 Callum Jones, Marta Martinez-Alonso, Hannah Gagg, Liam Kirby, Julia A. Weinstein, Helen E. Bryant
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The New Frontier: Merging Molecular Glue Degrader and Antibody–Drug Conjugate Modalities To Overcome Strategic Challenges J. Med. Chem. (IF 6.8) Pub Date : 2024-09-04 Yam B. Poudel, Ruchita R. Thakore, Eugene P. Chekler
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Discovery of a Highly Potent and Selective Inhibitor Targeting Protein Lysine Methyltransferase NSD2 J. Med. Chem. (IF 6.8) Pub Date : 2024-09-04 Jianwei Wei, Qiongyu Shi, Bang Li, Hong Yang, Li Liu, Ruilin Zhou, Zongbo Feng, Zhenjiao Yang, Jinhong Zhan, Xiao-Feng Xiong, Xun Huang, Yuanxiang Wang
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A Glycyrrhizin Derivative with a More Potent Inhibitory Activity against High-Mobility Group Box 1 Efficiently Discovered by Chemical Synthesis Inspired by the Bioconversion Products of an Endophytic Fungus Isolated from Licorice J. Med. Chem. (IF 6.8) Pub Date : 2024-09-04 Aoi Machida, Kengo Banshoya, Akiho Miyamaru, Tamaki Eto, Shoji Maehara, Yuhzo Hieda, Toshiyuki Hata, Masatoshi Ohnishi
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Heat Shock Protein 90 Interactome-Mediated Proteolysis Targeting Chimera (HIM-PROTAC) Degrading Glutathione Peroxidase 4 to Trigger Ferroptosis J. Med. Chem. (IF 6.8) Pub Date : 2024-09-04 Jinyun Dong, Furong Ma, Maohua Cai, Fei Cao, Haobin Li, Hui Liang, Yulong Li, Guangyu Ding, Juan Li, Xiangdong Cheng, Jiang-Jiang Qin
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Rational Design, Synthesis, and Structure–Activity Relationship of a Novel Isoquinolinone-Based Series of HBV Capsid Assembly Modulators Leading to the Identification of Clinical Candidate AB-836 J. Med. Chem. (IF 6.8) Pub Date : 2024-09-04 Andrew G. Cole, Steven G. Kultgen, Nagraj Mani, Kristi Yi Fan, Andrzej Ardzinski, Kim Stever, Bruce D. Dorsey, Eugen F. Mesaros, Emily P. Thi, Ingrid Graves, Sunny Tang, Troy O. Harasym, Amy C. H. Lee, Andrea Olland, Robert K. Suto, Michael J. Sofia
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Discovery and Optimization of N-Heteroaryl Indazole LRRK2 Inhibitors J. Med. Chem. (IF 6.8) Pub Date : 2024-09-04 Kaitlyn M. Logan, Will Kaplan, Vladimir Simov, Hua Zhou, Derun Li, Luis Torres, Gregori J. Morriello, John J. Acton, Barbara Pio, Yi-Heng Chen, Mitchell H. Keylor, Rebecca Johnson, Solomon D. Kattar, Ryan Chau, Xin Yan, Michael Ardolino, Cayetana Zarate, Karin M. Otte, Rachel L. Palte, Tina Xiong, Spencer E. McMinn, Shishi Lin, Santhosh F. Neelamkavil, Ping Liu, Jing Su, Laxminarayan G. Hegde, Janice
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Re-Evaluating PIN1 as a Therapeutic Target in Oncology Using Neutral Inhibitors and PROTACs J. Med. Chem. (IF 6.8) Pub Date : 2024-09-04 Chuan Liu, Zhonghui Chen, Tao Chen, Hongmei Song, Jianbo Shen, Xiaoxi Yuan, Shuai Xia, Qian Liu, Qiuxia Chen, Qiang Tian, Xiaoyun Meng, Zhu Han, Xiaofei Dong, Yu Yang, Longying Cai, Xuemin Cheng, Yangyang Jia, Guansai Liu, Jin Li, Junyou Ge, Dengfeng Dou
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Natural Product-Inspired Discovery of Naphthoquinone-Furo-Piperidine Derivatives as Novel STAT3 Inhibitors for the Treatment of Triple-Negative Breast Cancer J. Med. Chem. (IF 6.8) Pub Date : 2024-09-03 Chengcheng Fan, Shengying Lou, Chenjun Shen, Jialing Liao, Hao Ni, Siyu Chen, Zhihui Zhu, Xueping Hu, Wei Xie, Huajun Zhao, Sunliang Cui
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A Cyclometalated Iridium(III) Complex Exerts High Anticancer Efficacy via Fatty Acid Beta-Oxidation Inhibition and Sphingolipid Metabolism Reprogramming J. Med. Chem. (IF 6.8) Pub Date : 2024-09-03 Cuiyan Lin, Huiling Wang, Keyu Chen, Shuangqiang Liu, Zhichen Mao, Zuyu Mo, Rizhen Huang, Ye Zhang, Wei Xie, Jianhua Wei, Junfei Jin
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Structural Optimization and Structure–Activity Relationship of 1H-Pyrazole-4-carboxylic Acid Derivatives as DNA 6mA Demethylase ALKBH1 Inhibitors and Their Antigastric Cancer Activity J. Med. Chem. (IF 6.8) Pub Date : 2024-09-03 Feng Li, Liang Xiong, Jian Zhang, Yinping Guo, Ke Xu, Zijie Xiong, Yuyang Wang, Shanmian Ji, Aiping Tong, Linli Li, Shengyong Yang
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Pyrazolone-Based Zn(II) Complexes Display Antitumor Effects in Mutant p53-Carrying Cancer Cells J. Med. Chem. (IF 6.8) Pub Date : 2024-09-02 Sonila Xhafa, Corrado Di Nicola, Alessia Tombesi, Riccardo Pettinari, Claudio Pettinari, Francesca Scarpelli, Alessandra Crispini, Massimo La Deda, Angela Candreva, Alessia Garufi, Gabriella D’Orazi, Agustín Galindo, Fabio Marchetti
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Structure-Based Design and Development of Phosphine Oxides as a Novel Chemotype for Antibiotics that Dysregulate Bacterial ClpP Proteases J. Med. Chem. (IF 6.8) Pub Date : 2024-09-02 Funing Lin, Mark F. Mabanglo, Jin Lin Zhou, Gursonika Binepal, Marim M. Barghash, Keith S. Wong, Scott D. Gray-Owen, Robert A. Batey, Walid A. Houry
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Discovery and Preclinical Profile of ALG-055009, a Potent and Selective Thyroid Hormone Receptor Beta (THR-β) Agonist for the Treatment of MASH J. Med. Chem. (IF 6.8) Pub Date : 2024-09-02 Koen Vandyck, David C. McGowan, Xuan G. Luong, Sarah K. Stevens, Andreas Jekle, Kusum Gupta, Dinah L. Misner, Sushmita Chanda, Vladimir Serebryany, Michael Welch, Haiyang Hu, Zhidan Lv, Caroline Williams, Klaus Maskos, Alfred Lammens, Antitsa D. Stoycheva, Tse-I Lin, Lawrence M. Blatt, Leonid N. Beigelman, Julian A. Symons, Pierre Raboisson, Jerome Deval
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Correction to “Optimization Efforts for Identification of Novel Highly Potent Keap1-Nrf2 Protein–Protein Interaction Inhibitors” J. Med. Chem. (IF 6.8) Pub Date : 2024-09-02 Kazuki Otake, Yoshinori Hara, Minoru Ubukata, Masafumi Inoue, Noboru Nagahashi, Dai Motoda, Naoki Ogawa, Yoshiji Hantani, Rie Hantani, Tsuyoshi Adachi, Akihiro Nomura, Keishi Yamaguchi, Mariko Maekawa, Hideaki Mamada, Takahisa Motomura, Motohide Sato, Kazuhito Harada
The correct email addresses for the two corresponding authors are as shown in this Addition/Correction. This article has not yet been cited by other publications.
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Corannulene Amino Acid-Derived Water-Soluble Amphiphilic Buckybowls as Broad-Spectrum Membrane Targeting Antibacterial Agents J. Med. Chem. (IF 6.8) Pub Date : 2024-08-30 Saroj Maji, Sariyah Akhtar, Sabyasachi Halder, Indranil Chatterjee, Devesh Pratap Verma, Neeraj Kumar Verma, Jyotshana Saroj, Deepanshi Saxena, Rahul Maitra, Juhi Sharma, Bhawana Sharma, Hidehiro Sakurai, Kalyan Mitra, Sidharth Chopra, Jimut Kanti Ghosh, Gautam Panda