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Fluorocyclopropyl-Containing Tacrine Derivatives as Potent and Selective Dual CDK2/CDK9 Inhibitors for the Treatment of Colorectal Cancer J. Med. Chem. (IF 6.8) Pub Date : 2025-11-15 Limeng Wu, Wenjie Liu, Xinyue Ning, Xinyu Li, Zhiya Wang, Zhenshu Li, Yiming Qi, Jiao Xiao, Xiangbo Xu, Xudong Gao, Xinhua Liu, Yingshi Zhang, Zihua Xu, Wenwu Liu, Yonghong Liu, Qingchun Zhao
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Structural Rationalization of IPMK Inhibitor Potency J. Med. Chem. (IF 6.8) Pub Date : 2025-11-14 Huanchen Wang, Stephen B. Shears, Raymond D. Blind
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Cell-Active Peptide Inhibitors of the FANCM-RMI Interaction J. Med. Chem. (IF 6.8) Pub Date : 2025-11-14 Lisa J. Alcock, Joshua Mills, Rohan Bythell-Douglas, Haritha Krishna Sudhakar, Chandrika Deshpande, Toby Passioura, Andrew J. Deans, Yu Heng Lau
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Discovery of Potent, Allosteric GSTO1 Covalent Inhibitors with a New Binding Mode J. Med. Chem. (IF 6.8) Pub Date : 2025-11-13 Yanli Sun, Fengying Zhang, Lixin Zhou, Yixuan Feng, Shuke Yang, Qiuxian Lu, Xin Yuan, Wenqing Hou, Biwei Liu, Zhixiang Guo, Lu Chen, Bo Peng, Xianzhen Yin, Yiwen Zhang, Jing Yang, Nan Chen, Wenchao Lu
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Selectivity Approaches in Therapeutic Antibody Design J. Med. Chem. (IF 6.8) Pub Date : 2025-11-13 Mariam Fouad
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Identification of Novel Benzopyridonyl Cyanovinylpyrimidines as Potential Broad-Spectrum Antibacterial Members J. Med. Chem. (IF 6.8) Pub Date : 2025-11-13 Yi-Min Tan, Yu-Jia Wei, Nisar Ahmad, Shao-Lin Zhang, Wei-Wei Gao, Cheng-He Zhou
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Structure-Directed Optimization of Ebselen Derivatives as Potent NDM-1 Inhibitors Reverses Meropenem Resistance J. Med. Chem. (IF 6.8) Pub Date : 2025-11-12 Yan Guo, Chenyu Liu, Wandong Liu, Chen Zhang, Zhiying Liu, Shengbiao Wan, Ximing Xu, Sheng Chen, Jiazhang Qiu
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Discovery and Biological Evaluation of Novel, Potent, and Orally Available CBLB Inhibitors J. Med. Chem. (IF 6.8) Pub Date : 2025-11-12 Fanye Meng, Zhongying Cao, Jinxin Liu, Yazhou Wang, Zhilin Ning, Jiaojiao Yu, Yaya Fan, Shan Chen, Man Zhang, Frank W. Pun, Alex Aliper, Feng Ren, Xin Cai, Xiao Ding, Alex Zhavoronkov
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H2S-Activated Theranostic Platform for Precise Photoablation of Colorectal Tumors with NIR-II Dual-Modal Phototherapy J. Med. Chem. (IF 6.8) Pub Date : 2025-11-12 Kehuan Wu, Lixin Sun, Hongyu Wu, Xinru Zheng, Yongxing Xue, Ziwen Zhang, Shaozong Ma, Chunchang Zhao, Yingchao Liu, Xianfeng Gu
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A Fragment-Based Electrophile-First Approach to Target Histidine with Aryl-Fluorosulfates: Application to hMcl-1 J. Med. Chem. (IF 6.8) Pub Date : 2025-11-12 Giulia Alboreggia, Kendall Muzzarelli, Zahra Assar, Maurizio Pellecchia
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Highly Specific Inhibition of c-Myc Oncogene Expression through Shifting the G-Quadruplex toward a Triplex Structure J. Med. Chem. (IF 6.8) Pub Date : 2025-11-12 Jolanta Lisowiec-Wąchnicka, Karolina Zielińska, Anna Pasternak
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Discovery of Novel Dihydroxyphenol Tyrosinase Inhibitors for Treatment of Pigmentation: From Enzyme Screening to Three-Dimensional Human Skin Melanin Evaluation J. Med. Chem. (IF 6.8) Pub Date : 2025-11-12 Jiahui Wang, Yinyan Sun, Xiaoying Jiang, Hao Wen, Hong Cai, Meiling Feng, Xiaotian Niu, Shan Wang, Jia Zhi, Junchao Xie, Rui Wang, Wenchao Chen, Renren Bai
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Mechanistic Characterization of a Small Molecule as a Direct NLRP3 Inhibitor via Binding to the NACHT Domain J. Med. Chem. (IF 6.8) Pub Date : 2025-11-12 Yiming Xu, Hallie Blevins, Savannah Biby, Jannatun N. Namme, Kun Zhang, Renfeng Li, Shijun Zhang
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Engineering of an Ultralong-Acting and Nonaggregating Dual Amylin and Calcitonin Receptor Agonist with Durable Efficacy in Obesity and Diabetes J. Med. Chem. (IF 6.8) Pub Date : 2025-11-12 Nan Zheng, Rongfang Chen, Luying Yang, Pu Xu, Xueying Wang, Xin Sun, Yanxia Lin, Jinying Qiu, Xiao-xuan Su, You Wang, Leiming Wang, Weijun Shen
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Quinoline-Based DNA Methyltransferase Inhibitors Featuring Basic Side Chains: Design, Synthesis, and Insight in Biochemical and Anticancer Cell Properties J. Med. Chem. (IF 6.8) Pub Date : 2025-11-11 Clemens Zwergel, Chiara Lambona, Rossella Fioravanti, Alessia Raucci, Francesco Fiorentino, Guilaine Nchugoua Tchieh, Corinne Jallet, Laurent Lacroix, Michela Pierrettori, Francesca Romana Pellegrini, Yan Xiong, Jian Jin, Paola Arimondo, Daniela Trisciuoglio, Antonello Mai, Sergio Valente
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Development of Petrelintide: a Potent, Stable, Long-Acting Human Amylin Analogue J. Med. Chem. (IF 6.8) Pub Date : 2025-11-11 Henrik Fischer Munch, Rasmus Just, Jesper Mosolff Mathiesen, Per-Olof Eriksson, Jesper Skodborg Villadsen, Bill Vestergaard, Maria Deryabina, Oliver Demmer, Jolanta Skarbaliene, Dieter W. Hamprecht, Wolfgang Rist, Tamara Baader-Pagler, Achim Grube, Alexander Heim-Riether, Lise Giehm
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Small Molecules Targeting the Transmembrane Domain J. Med. Chem. (IF 6.8) Pub Date : 2025-11-11 Yibo Wang, Xiaohui Wang
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A New Era for PPARγ: Covalent Ligands and Therapeutic Applications J. Med. Chem. (IF 6.8) Pub Date : 2025-11-11 Jasmine L. King, Luke Smithers, Alice Vrielink, W. Joost Lesterhuis, Matthew J. Piggott
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Design, Synthesis, and Anti-inflammatory Activity Evaluation for Hydrazide-Based HDAC6 Targeted Protein Degraders J. Med. Chem. (IF 6.8) Pub Date : 2025-11-11 Simin Sun, Kairui Yue, Enqiang Liu, Danmei Sheng, Yuxin Chen, Tianqi Li, Aijun Shen, Geng Jia, Yuqi Jiang, Xiaoyang Li
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N-Aryl-N-Lactosylamides as Potent and Highly Selective Inhibitors of Galectin-3 with Antifibrotic Activity J. Med. Chem. (IF 6.8) Pub Date : 2025-11-11 Jakub Zýka, Jaroslav Kozák, Lenka Vanekova, Marketa Pimkova Polidarova, Vít Prouza, Nina Habanová, Timotej Strmeň, Martin Zavřel, Petr Pachl, Jan Choutka, Klara Grantz Saskova, Andrea Brazdova, Kamil Parkan, Radek Pohl
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Rational Design and Biological Evaluation of a Novel Polθ Polymerase Inhibitor for Synergistic Targeting of HR-Deficient Cancers J. Med. Chem. (IF 6.8) Pub Date : 2025-11-10 Ziheng Yu, Zhen Li, Lei Jiang, Yibin Zhang, Jingxue Zhang, Lu Liu, Ying Qu, Yuchen Wei, Mengying Li, Tao Lu, Zhengtao Li, Yadong Chen, Jie Feng
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Design and Synthesis of Novel N-(1H-pyrazol-3-yl)pyrimidin-4-amine Aurora/HDAC Dual Inhibitors for Colorectal Cancer Treatment J. Med. Chem. (IF 6.8) Pub Date : 2025-11-10 Hao Cui, Xu Huang, Rui Li, Meng Zong, Shilong Sun, Hongmei Li, Yadong Chen, Tao Lu, Yong Zhu
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LEKTI-Grafted Sunflower Trypsin Inhibitor: A Potential Therapeutic for Skin Diseases J. Med. Chem. (IF 6.8) Pub Date : 2025-11-10 Jeffrey Mah, Vignesh Jayarajan, Xin Huang, Wei-Li Di, Derek Macmillan
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Kill Two Birds with One Stone: An Efficient and Potent AR CBS-Targeted Degrader Reverses Breast Cancer Resistance via Concurrent AR Degradation and ERα Transcriptional Suppression J. Med. Chem. (IF 6.8) Pub Date : 2025-11-10 Yihe Wu, Baohua Xie, Jinsen Liang, Dongmei Wei, Yubo Wang, Yudong Yin, Xiaofei Deng, Chao Wang, Jian Ni, Lanxin Yang, Chune Dong, Xin Han, Hai-Bing Zhou
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Pt(IV) Prodrugs Bearing Sunitinib-Derived Ligands Display Exceptional Anticancer Activity against Renal Cell Carcinoma When Compared to Conventional Platinum Chemotherapy J. Med. Chem. (IF 6.8) Pub Date : 2025-11-10 Darren F. Beirne, Jemma Arakelyan, Matteo Forner, Ho-Jung Choe, Kirill Kriukov, Eithne Dempsey, Valentina Gandin, Trinidad Velasco-Torrijos, Maria V. Babak, Diego Montagner
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Antibacterial Benzimidazole-2-Methanamines as Allosteric Modulators of Streptococcus pneumoniae Penicillin-Binding Protein 2x J. Med. Chem. (IF 6.8) Pub Date : 2025-11-10 Homero Dominguez-Cisneros, Mohini Mohan Konai, Choon Kim, Neha Rana, Rhona Feltzer, Jeshina Janardhanan, Amr M. El-Araby, Van T. Nguyen, Jed F. Fisher, Mayland Chang, Shahriar Mobashery
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FDA Drug Repurposing Uncovers Modulators of Dopamine D2 Receptor Localization via Disruption of the NCS-1 Interaction J. Med. Chem. (IF 6.8) Pub Date : 2025-11-10 Daniel Muñoz-Reyes, Lorena Aguado, Sandra Arroyo-Urea, Carlos Requena, Sara Pérez-Suárez, Sonia Sánchez-Yepes, Josep Argerich, Celia Miró-Rodríguez, Eugenia Ulzurrun, Eulalia Rodríguez-Martín, Javier García-Nafría, Nuria E. Campillo, Alicia Mansilla, María José Sánchez-Barrena
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Multisite Occupancy and Multidimensional Optimization: Design and Evaluation of Piperazine-Thioureidobenzamide Derivatives as Potent HBV Capsid Assembly Modulators J. Med. Chem. (IF 6.8) Pub Date : 2025-11-10 Minghui Liang, Yutong Dou, Jian Zhang, Zechun Yang, Yuanyuan Liu, Mei Wang, Yiyan Mao, Lindan Guan, Aixin Li, Yuqing Cai, Yan Wang, Peng Xue, Lei Zhang, Zhuanchang Wu, Xinyong Liu, Peng Zhan, Haiyong Jia
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Phenotypic Hit Identification and Optimization of Novel Pan-TEAD and Subtype-Selective Inhibitors J. Med. Chem. (IF 6.8) Pub Date : 2025-11-10 Timo Heinrich, Alessia Gambardella, Daniel Schwarz, Carl Petersson, Jakub Gunera, Sakshi Garg, Richard Schneider, Marina Keil, Lisa Grimmeisen, Andrea Unzue Lopez, Heike Schilke, Thomas Weitzel, Christian Kolb, Patrizia Diehl, Benjamin Doerfel, Uwe Anlauf, Vivian Reither, Corinna Rettig, Beate Opelt, Andrea Delp, Nicole Wildner, Djordje Musil, Erik Friedrich, Lars Burgdorf, Thomas Fuchss, Lisa Albers
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Potent Preorganized Pyrazolidine Cyclophilin D Inhibitors Prevent Mitochondrial and Organ Injury in a Mouse Pancreatitis Disease Model J. Med. Chem. (IF 6.8) Pub Date : 2025-11-09 Muhammad Awais, Christopher M. Woodley, Liqun Guo, Michael Rogers, Neil Kershaw, Thomas Zacharchenko, Emma Shore, Arjun Kattakayam, Rajarshi Mukherjee, David N. Criddle, Suet C. Leung, Heather Lee, Joshua Burgess-McCann, Konstantin Luzyanin, Neil G. Berry, Svetlana Antonyuk, Lu-Yun Lian, Robert Sutton, Paul M. O’Neill
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Discovery of Novel Potent and Safe Immunoproteasome Inhibitors with Bridged Ring for Anti-Inflammatory Therapy J. Med. Chem. (IF 6.8) Pub Date : 2025-11-09 Jian Wu, Shi Cai, Jincai Su, Xiaojun Ji, Qiuhua Zhou, Zehong Chen, Yiqing Fan, Xuefei Li, Jiang Liu, Wanting Dong, Changyou Ma, Dan Xu, Hai Qian
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Crizotinib- or Ceritinib-Conjugated Platinum(IV) Prodrugs As Potent Multiaction Agents Inducing Antiproliferative Effects in 2D and 3D Cancer Cell Models J. Med. Chem. (IF 6.8) Pub Date : 2025-11-09 Sofia Sharkawy, Sourav Acharya, Hana Kostrhunová, Moumita Maji, Lenka Marková, Vojtěch Novohradský, Dan Gibson, Viktor Brabec
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Phytohormone Strigolactams Overcomes Oxaliplatin Resistance in Colorectal Cancer by Blocking the Late-Stage Autophagy to Tip the Metabolic Balance toward Ferroptosis J. Med. Chem. (IF 6.8) Pub Date : 2025-11-09 Tingting Liu, Xingyue Chen, Shah Nawaz Khan, Xiaoxu Li, Bo Kong, Yingjun Zhou, Yangyan Li, Yuhua Ge, Gang Chen, Xu Deng
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Targeting Protein Tyrosine Phosphatase Nonreceptor Type 2 with a Novel Inhibitor for the Treatment of Melanoma J. Med. Chem. (IF 6.8) Pub Date : 2025-11-08 Wenbin Kuang, Qiannan Li, Wenmu Wang, Dawei Wang, Chen Tong, Mingge Song, Kailin Han, Jianing Liu, Anyan Chen, Ya Chen, Liping Wang, Haiping Hao, Xiao Wang, Yibei Xiao, Peng Yang
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Novel Pyridine-Based Fibroblast Activation Protein-Targeted Tracers: Design, Synthesis, and PET Imaging Evaluation for Tumors J. Med. Chem. (IF 6.8) Pub Date : 2025-11-07 Ziyue Yu, Yong Huang, Zeng Jiang, Hualong Chen, Xuebo Cheng, Yajing Liu, Ying Liang, Zehui Wu
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Discovery of a “First-in-Class” Selective Multikinase (CDK4/6/9-AURKA/B) Inhibitor, LCI133, for Neuroblastoma J. Med. Chem. (IF 6.8) Pub Date : 2025-11-06 Krishnaiah Maddeboina, Dhananjaya Pal, Bharath Yada, Cody C. McHale, Sandeep K. Singh, Yashpal S. Chhonker, Hailey L. Dryden, Ritchie Delara, Vaidehi Mujumdar, Qi Zhang, Daryl J. Murry, Donald L. Durden
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Backbone Alterations in Cyclic Peptides Influence Both Membrane Permeability and Biological Activity J. Med. Chem. (IF 6.8) Pub Date : 2025-11-06 Joseph Openy, Sabela Vega-Ces, Gulshan Amrahova, Emeline Mestdach, Celestine Chi, Benjamin Kissel, Peter ‘t Hart
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Novel Dimeric Capsid Assembly Modulators as a Unique Class of Highly Potent Anti-HBV Agents J. Med. Chem. (IF 6.8) Pub Date : 2025-11-06 Franck Amblard, Zhe Chen, Kalouna Kra, Dharmeshkumar Patel, Leda Bassit, Laetitia Gargowitsch, Jéril Degrouard, Virgile rat, Ana-Andreea Arteni, Lauren Matthews, Shreya M. Ravichandran, Alfred Jiang, Antonis Athanasiadis, Georgios Dangas, Maedot Abate, Guillaume Tresset, Julien Pronost, Mohammad Salman, Kiran Verma, Karen A. Kirby, Eleftherios Michailidis, Hugues de Rocquigny, David Durantel, Stéphane
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Discovery and Optimization of a Non-Nucleoside-Based Series of Inhibitors of 2′-Deoxynucleoside 5′-Monophosphate Glycosidase (DNPH1) J. Med. Chem. (IF 6.8) Pub Date : 2025-11-05 Bernard Barlaam, Luz Alonso-Crisostomo, Niall A. Anderson, Argyrides Argyrou, Peter C. Astles, Elaine B. Cadogan, Luca Carlino, Gavin W. Collie, Nichola L. Davies, James Hall, Linda Kitching, Xianxi Li, Filippos Michopoulos, Alexander G. Milbradt, Jenni Nikkilä, Sarah Northall, Mark J. O’Connor, Xiaohiu Pei, Joseph Shaw, Danial Slade, Harriet Southgate, Darren Stead, Christopher J. Stubbs, Benjamin
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Structure-Based Design of a Highly Potent Dual-Competitive FTO Inhibitor for Targeted m6A Demethylase Inhibition in AML J. Med. Chem. (IF 6.8) Pub Date : 2025-11-05 Xi Zhang, Zhen Wang, Xinyun Xie, Gege Liu, Ze Dong, Cai-Guang Yang
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Structure-Informed Design of High-Cooperativity PROTAC Targeting SARS-CoV-2 RdRp via Click Chemistry and Enhanced Sampling Simulations J. Med. Chem. (IF 6.8) Pub Date : 2025-11-04 Kiran Shehzadi, Yue Ran, Iqra Kalsoom, Jingyue Dong, Peifeng Gao, Irfan Muhammad, Ming-Jia Yu, Zihui Meng, Jian-Hua Liang
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Sulfonation Disposition of Capsaicin: In Vitro and in Vivo J. Med. Chem. (IF 6.8) Pub Date : 2025-11-04 Xiaohuan Dou, Shan Wang, Qidong Zhang, Jian Mao, Guobi Chai, Qingzhao Shi, Yunhe Zhu, Wu Fan
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Synthesis and Pharmacological Characterization of Nociceptin/Orphanin FQ Dimeric Ligands J. Med. Chem. (IF 6.8) Pub Date : 2025-11-04 Valentina Albanese, Pietro Pola, Michela Argentieri, Tiziano De Ventura, Alessia Frezza, Davide Illuminati, Davide Malfacini, Erika Marzola, Giulio Meneguzzo, Erika Morrone, Delia Preti, Alessandra Rizzo, Chiara Sturaro, Girolamo Calò, Remo Guerrini, Salvatore Pacifico, Chiara Ruzza
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Rational Leucine-Centric Design Confers Enhanced Proteolytic Stability and Reduced Toxicity of Antimicrobial Peptides against Multidrug-Resistant Bacterial Infections J. Med. Chem. (IF 6.8) Pub Date : 2025-11-04 Shuyuan Jiang, Wenpeng Zhang, Long Tian, Chunlan Zeng, Jiaqi Han, Xia Wu, Yijie Xu, Longming Chen, Jiangmin Zeng, Chunhui Zhao, Li Zhang, Liang Luan, Weifeng Ye, Changhao Zhang, Taoran Wang, Qingbin Meng
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Application of Hypoxia-Activated Prodrugs in Tumor Therapy: Design Strategies and Perspectives J. Med. Chem. (IF 6.8) Pub Date : 2025-11-04 Shengyu Liu, Mijia Zhang, Xiangxi Sun, Peng Wang, Guogang Zhang, Wenyan Li
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Lactucopicrin: A Sesquiterpene Lactone with Anti-Inflammatory Activity Modulates the Crosstalk between NF-kB and AHR Pathways J. Med. Chem. (IF 6.8) Pub Date : 2025-11-04 María Ángeles Ávila-Gálvez, Catarina J G Pinto, Carlos Rafael-Pita, Inês P. Silva, Aleksandra T. Janowska, Sérgio Marinho, Rory Saitch, Yilong Lian, Pakavarin Louphrasitthiphol, Jonas Protze, Gerd Krause, Pedro Moura-Alves, Cláudia Nunes dos Santos
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Use of Direct-to-Biology Strategies for the Discovery of 2′-Deoxynucleoside 5′-Monophosphate N-Glycosidase (DNPH1) PROTACs J. Med. Chem. (IF 6.8) Pub Date : 2025-11-03 Niall A. Anderson, Bernard Barlaam, Argyrides Argyrou, Peter C. Astles, Hanna Bruss, Elaine B. Cadogan, Luca Carlino, Luz Alonso-Crisostomo, Gavin W. Collie, Alex J. Edwards, Anastasiia Gryniukova, James Hall, Kunzah Jamal, Joshua Kent, Linda Kitching, Christopher Kourra, Carolyn Lam, Alexander G. Milbradt, Jenni Nikkilä, Sarah Northall, Mark J. O’Connor, Jeroen Overman, Claudio Pathe, Wendy Savory
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Design, Syntheses, and Pharmacological Evaluations of Core Ring Expanded Fentanyl Analogues as Potential Counteracting Agents Against Fentanyl Induced Respiratory Depression J. Med. Chem. (IF 6.8) Pub Date : 2025-11-03 Abeje A. Silte, Ennian Li, Balaji S. Kale, Logan Neel, Neha Upadhyay, Rachael Flammia, Rui Lyu, Celsey M. St Onge, Ahmed Reda, Samuel Woodard, James C. Gillespie, Daniel Kim, Dana E. Selley, William L. Dewey, Piyusha P. Pagare, Yan Zhang
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Discovery of Novel P2Y14R Inhibitors for Ameliorating Liver Fibrosis by Suppressing Hepatic Stellate Cell Activation J. Med. Chem. (IF 6.8) Pub Date : 2025-11-03 Chencheng Li, Hui Wang, Li Liu, Chunxiao Liu, Yiyun Wang, Li Yin, Yalian Yang, Sheng Tian, Jialong Qian, Mengze Zhou, Huanqiu Li, Qinghua Hu
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A Comparative Study on the Effect of Near-Infrared Fluorescent Dyes on the Pharmacokinetic Behavior of Nanobody-Based Tracers for In Vivo Imaging J. Med. Chem. (IF 6.8) Pub Date : 2025-10-31 Noemi B. Declerck, Sofie Declercq, Pieterjan Debie, Julie Du Ville, Łukasz Mateusiak, Jelena Saliën, Marcus C. M. Stroet, Michael P. Luciano, Dong-Hao Li, Martin J. Schnermann, Bradley D. Smith, Sophie Hernot
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Design, Synthesis, and Evaluation of a Novel 99mTc-Labeled Small Molecule Inhibitor (Lapatinib)-Based SPECT Tracer Targeting HER2 J. Med. Chem. (IF 6.8) Pub Date : 2025-10-31 Zuojie Li, Lina Diao, Peiwen Han, Qingna Xiao, Dajie Ding, Junhong Feng, Jianyong Jiang, Junbo Zhang
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Three in One: Viscosity-Sensitive Ruthenium(II) Complexes for Photodynamic Anticancer by Activating Pyroptosis with Self-Evaluation Therapeutic Efficacy and Two-Photon Imaging J. Med. Chem. (IF 6.8) Pub Date : 2025-10-30 Xiurong Ma, Guixi Wang, Qian Zhou, Yanxiong Liu, Runying He, Zuoxun Xie, Yonggang Shi, Qiue Cao, LiYan Zheng
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Rational Design of PROTAC Degraders and Their Spatiotemporal Controlled Delivery for Enhanced Tumor Penetration and PD-L1 Protein Degradation J. Med. Chem. (IF 6.8) Pub Date : 2025-10-30 Qianqian Qi, Zhanyu Zhang, Xiang ji, Dun Wang
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Discovery of Highly Potent and Orally Available CCNK Molecular Glue Degraders as Broad-Spectrum Antitumor Agents J. Med. Chem. (IF 6.8) Pub Date : 2025-10-30 Yuxia Liu, Zhongcheng Yang, Zibin Liao, Suchang Chen, Zhihong Qin, Zhiling Liang, Lianru Chen, Chu Bao, Min Wei, Luyong Zhang, Zheng Li
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Discovery of Clinical Candidate GDC-8264, a Novel, Potent and Selective RIP1 Inhibitor for Amelioration of Tissue Damage and the Treatment of Inflammatory Diseases J. Med. Chem. (IF 6.8) Pub Date : 2025-10-30 Snahel Patel, Huifen Chen, Eugene Varfolomeev, Youngsu Kwon, Sreemathy Ramaswamy, Pawan Bir Kohli, John G. Quinn, Joshua D. Webster, Jialin Mao, Yuan Chen, Rina Fong, F. Esra Demircioglu, Patrick Lupardus, Craig Stivala, Gregory L. Hamilton, Michael Siu, Swathi Sujatha-Bhaskar, Vishnu Mohanan, Adeyemi O. Adedeji, Sara F. Santagostino, Jonathan Maher, Brent McKenzie, Michael E. Rothenberg, Adam Johnson
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Therapeutic Potential of 2,2′:6′,2″-Terpyridine-Based Au(III), Pt(II), and Mn(II) Complexes against 2D and 3D Human Colorectal Resistant Cancer Cells J. Med. Chem. (IF 6.8) Pub Date : 2025-10-30 Katarzyna Choroba, Barbara Machura, Mateusz Penkala, Karol Erfurt, Sandra Cordeiro, Vanessa Araújo, Edvânia Leopoldo, Rute Lima, Diogo Afonso, Pedro V. Baptista, Alexandra R. Fernandes
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Correction to “Identifying Artifacts from Large Library Docking” J. Med. Chem. (IF 6.8) Pub Date : 2025-10-30 Yujin Wu, Fangyu Liu, Isabella Glenn, Karla Fonseca-Valencia, Lu Paris, Yeyue Xiong, Olivier Mailhot, Steven V. Jerome, Charles L. Brooks, III, Brian K. Shoichet
We inadvertently left an author, Dr. Olivier Mailhot, off the version of the paper we published in the Journal of Medicinal Chemistry. We are adding Dr. Mailhot as a middle author; Dr. Mailhot was responsible for creating Figure 1 of the accepted paper. We are also correcting the name of Dr. Xiong, which in the published paper was written as Yuyue Xiong, but it should be Yeyue Xiong. We are making
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Correction to “Sebetralstat (KVD900): A Potent and Selective Small Molecule Plasma Kallikrein Inhibitor Featuring a Novel P1 Group as a Potential Oral On-Demand Treatment for Hereditary Angioedema” J. Med. Chem. (IF 6.8) Pub Date : 2025-10-30 Rebecca L. Davie, Hannah J. Edwards, D. Michael Evans, Simon T. Hodgson, Michael J. Stocks, Alun J. Smith, Louise J. Rushbrooke, Stephen J. Pethen, Michael B. Roe, David E. Clark, Paul A. McEwan, Sally L. Hampton
In the Results and Discussion section, under the subheading Characterization of the Clinical Candidate 14w, the sentence reads “Sebetralstat, 14w, is a potent, competitive, and reversible inhibitor of human PKa (Ki = 3.0 nM) with fast kinetics (kon >10 × 106 M–1 s–1).” Instead, the unit of the association constant for sebetralstat should be corrected and reported as “kon >10 × 10–6 M–1 s–1”. This article
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Discovery of (4-Phenyl-cyclohexyl)acetate-Derived Tyrosylprotein Sulfotransferase 2 (TPST2) Inhibitors with Potent Anti-Tumor Activity for Immuno-Oncology Applications J. Med. Chem. (IF 6.8) Pub Date : 2025-10-30 Soo Bin Park, Hyun Kim, Yumi Oh, Minwoo Jin, Myeonggil Jeon, Yunjae Kim, Taein Park, Jihyun Kim, Beomki Cho, Chaemin Noh, Jihyeok Cho, Je-Heon Lee, Chanyeong Jeong, Ji-Woo Mok, Soo Hyun Eom, Sung-Yup Cho, Hansoo Park, Yong-Chul Kim
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Structure-Based Generation of 3D Small-Molecule Drugs: Are We There Yet? J. Med. Chem. (IF 6.8) Pub Date : 2025-10-29 Bo Yang, Chijian Xiang, Tongtong Li, Yunong Xu, Jianing Li
更新日期：2025-11-14
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