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“BRAF Inhibitors in Melanoma: Structural Insights, Therapeutic Resistance, and Biological Evaluation of Quinazoline Derivatives.” Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-06-11 Arghya Paik, Gurubasavaraja Swamy Purawarga Matada, Abhishek Ghara, Rohit Pal, Gajjala Pavani, Hemalatha Kamurthy
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PET Imaging of the Opioid System Using Radioligands: Synthetic Approaches and Translational Applications. Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-06-11 Carlo Reale, Giuliana Costanzo, Giuseppe Cosentino, Carmela Parenti, Lorella Pasquinucci
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Design of spiro-heterocyclic substituted diaminonaphthalene Keap1-Nrf2 protein-protein interaction inhibitors as novel anti-depressant agents Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-06-08 Yitong Chen, Qingqing Qin, Wenxin Ding, Ruizhi Yu, Rui Wang, Hualong Ji, Jianyu Yan, Hao Ma, Cheng-Shi Jiang, Yi Sun, Chunlin Zhuang
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Novel trimethyl lock-based prostate-specific membrane antigen targeted Conjugates: Design, synthesis, and biological activity evaluation Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-06-09 Jiangzhu Zhan, Lijun Xu, Shuaibing Ding, Ning Ding, Wei Zhang
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Corrigendum to “Synthesis and clinical application of new drugs approved by NMPA in 2023” [European Journal of Medicinal chemistry 283 (2025) 117181/EJMECH-d-24-03758] Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-06-11 Lijuan Xie, Yingying Wang, Kunyu Wang, Wanying Chen, Fuwei Yang
The authors regret < insert corrigendum text>.
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Bacterial cytidine deaminases as versatile activators of fluoropyrimidine nucleoside prodrugs Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-06-10 Viktorija Preitakaitė, Arūnas Kazlauskas, Agota Aučynaitė, Kamilė Butkutė, Ringailė Lapinskaitė, Nina Urbelienė, Audrius Laurynėnas, Rolandas Meškys
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Design, synthesis, and biological evaluation of caffeic acid-based novel multifunctional molecules for the management of Alzheimer's disease Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-06-10 Sunil Kumar, Gyan Modi
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AR-A014418-based dual Glycogen Synthase Kinase 3β / Histone Deacetylases inhibitors as potential therapeutics for Alzheimer’s disease Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-06-10 Alan Santini, Elisa Tassinari, Alessandra Altomare, Manuela Loi, Elisabetta Ciani, Stefania Trazzi, Rebecca Piccarducci, Simona Daniele, Claudia Martini, Barbara Pagliarani, Andrea Tarozzi, Matteo Bersani, Francesca Spyrakis, Daniela Danková, Eleonora Poeta, Simone Raimondi, Lara Davani, Giancarlo Aldini, Vincenza Andrisano, Angela De Simone, Andrea Milelli
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Syntheses of benzothiazole amidoximes and arylimidamides and evaluation of their ADME and DNA binding properties and activity against Trypanosoma brucei Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-06-07 Valentina Rep Kaulić, Martina Piškor, Sanja Koštrun, Astrid Milić, Marijana Radić Stojković, Amanda Fortes Francisco, Martin C. Taylor, John M. Kelly, Silvana Raić-Malić
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Design, synthesis and evaluation of anti-heart failure activity of O-glucoside derivatives Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-06-10 Yu Liu, Heng Liu, Xutong Wang, Bing Wang, Xiaodong Fang, Qiming Li, Meng Sun, Kejing Ma, Zeyu Gao, Yong Zhang, Weina Han
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Design, synthesis, and biological evaluation of novel PI3Kδ/HDAC6 dual inhibitors for the treatment of non-Hodgkin’s lymphoma Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-06-09 Yueqi Zuo, Yongxia Zhu, Peng Luo, Nan Huang, Kun Yao, Ke Zhang, Ningyu Wang, Xingchun Gou
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Design, synthesis, and biological evaluation of novel pyridazinone-based EED inhibitors for prostate cancer Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-06-09 Zhang-Xu He, Shi-xuan Tan, Zengyangzong Dan, Guan-jun Dong, Yu-lin Liu, Li-Ying Ma, Wen Zhao
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Novel water-soluble and highly efficient dual type I/II next generation inhibitors of FMS-like tyrosine kinase 3 (FLT3) Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-06-08 Andreas Sellmer, Marina Able, Karsten Spiekermann, Maria Reinecke, Bernhard Kuster, Kirsten Utpatel, Lukas Wirth, Herwig Pongratz, Nicole Plank, Pierre Koch, Sigurd Elz, Amrei Fischer, Belay Tizazu, Heinz-Herbert Fiebig, Stefan Dove, Siavosh Mahboobi
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NQO1 Induction and Radiation-Based Biodistribution Study of a New Quinoline Derivative Identified in a Screen of 6,8-Diiodoquinazolinone Sulfonamide Conjugates Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-06-07 Aiten M. Soliman, Mostafa M. Ghorab, Maureen Higgins, Albena T. Dinkova-Kostova, Mohamed Korany, Mohamed A. Amin, Mohammed A. Khedr, Tamer M. sakr
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Heterocyclic androstane derivatives targeting hormone-related cancers: Synthesis, bioactivity and docking studies Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-06-06 Tijana Lj. Šestić, Sofija S. Bekić, Maja A. Marinović, Marie Kvasnicová, Tereza Štenclová, Lucie Rárová, Andjelka S. Ćelić, Edward T. Petri, Jovana J. Ajduković, Miroslav Strnad, Marina P. Savić
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Indo–Gem: An Activatable Theranostic Prodrug, a “Turn–On” Fluorescent Probe, and a Targetable Imaging Agent in the Zebrafish Gallbladder System Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-06-04 Neha Jain, Arkaprava Roychaudhury, JunHyuk Kim, Ruchi Dixit, Prasad M. Sonawane, Michio Iwaoka, Cheol–Hee Kim, Satish Balasaheb Nimse, David G. Churchill
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Corrigendum to “Design, synthesis, and biological evaluation of novel BTK-targeting proteolysis targeting chimeras (PROTACs) with enhanced pharmacokinetic properties” [Eur. J. Med. Chem. 289 (2025) 117420] Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-06-04 Ying Lin, Jing Liu, Xinjian Tian, Jin Wang, Huahua Su, Jianpin Xiang, Tao Cao, Yonghui Wang, Qiong Xie, Xufen Yu
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A medicinal chemistry perspective on ATR: Current status and future directions Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-06-02 Kun Li, Xiangxi Sun, Shengyu Liu, Yidong Liu, Xue Feng, Guogang Zhang
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Discovery of an ALK degrader for lorlatinib-resistant compound mutations Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-06-02 Fei Gao, Zhenhua Wu, Anqi Lin, Xinyu Wu, Baoding Zhang, Liqing Liu, Yue Lu, Shangshang Geng, Zhen Huang, Yiyu Chen, Jianming Zhang, Li Li, Xianming Deng
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An exploration of molecular signaling in drug reprocessing for Oral Squamous Cell Carcinoma Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-05-31 Ali Nakhaei, Sarah Marzoughi, Sahar Ghoflchi, Hossein Hosseini, Amir R. Afshari, Mohammad Jalili-Nik, Prashant Kesharwani, Amirhossein Sahebkar
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PSMA targeted Therapy: From molecular mechanisms to clinical breakthroughs in castration-resistant prostate cancer Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-05-30 Licheng Wang, Change Lu, Xin'an Wang, Denglong Wu
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Innovative zinc-binding inhibitors of Legionella pneumophila ProA reduce collagen and flagellin degradation, TLR5 evasion, and human lung tissue inflammation Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-05-30 Lina Scheithauer, Camilla Ornago, Jolanda Selmar, Christian Schütz, Gabriele Bianchi, AlexanderF. Kiefer, Jörg Haupenthal, Ansgar Dellmann, DucT. Huynh, Ruoyu Zhang, Wulf Blankenfeldt, AnnaK.H. Hirsch, Michael Steinert
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Discovery and SAR Exploration of Novel Nanomolar 3,4-dihydroquinazolin-2(1H)-one Non-Nucleoside Reverse Transcriptase Inhibitors Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-05-29 Eline Goffin, Laurynn Torfs, Fanos Tsingis, David Švestka, Kristien Erven, Kris Uyttersprot, Cindy Heens, Simon Wilms, Jef Rozenski, Eveline Lescrinier, Christophe Pannecouque, Peter Verwilst
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Mechanistic Analysis of Diverse Click reactions along with their Applications Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-05-28 Sushmita Bhatia, Avadh Biharee, Souren Mondal, Swanand Kulkarni, Rakesh Kumar, Suresh Thareja
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Picomolar bivalent inhibitors of protein kinase CK2 active against β-coronavirus replication Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-05-29 Dylan Grenier, Dennis Salomon Lopez Molina, Muriel Gelin, Angélique Mularoni, Jean-François Guichou, Jean-Guy Delcros, Charlotte Martinasso, Yinshan Yang, Nazim Ahnou, Jean-Michel Pawlotsky, Abdelhakim Ahmed-Belkacem, Isabelle Krimm
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A new insight into cardiovascular protective potentials of hydroxylated xanthones Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-05-29 Lai Yen Fong, Hee Yang Derrick Cheow, Chin Theng Ng, Yoke Keong Yong, Yang Mooi Lim, Siau Hui Mah
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Discovery of indane and naphthalene derivatives as USP7 inhibitors Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-05-29 Xian Zhang, Shudan Tan, Dalin Wang, Huayun Zhu, Di Chen, Yueting Chen, Guangqing Wu, Zhizhen Zhu, Fengyi Zhang, Zijiang Liang, Li Xu, Xing Li, Haoliang Yuan, Qinglong Xu, Liang Dai, Zhiqi Feng, Caiping Chen, Liu Liu, Xiaoan Wen
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Discovery of highly potent naphthalene/quinoline-based PAD inhibitors: Structure-activity relationship, selectivity, and cytotoxicity Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-05-29 Yijiang Jia, Sina Bahraminejad, Xin Duan, Sydney Kong, Ayijiang Taledaohan, Chenyao Jiang, Dejian Ma, Jianxiong Jiang, Yuji Wang, Jiawang Liu
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Discovery and structure-activity relationship studies of 3-pyridazinesulfonyl derivatives as a new class of inhibitors against NLRP3 inflammasome-dependent pyroptosis Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-05-29 Jinshan Nan, Shanmian Ji, Nenghua Zhou, Yan Jiao, Yun Zhang, Shengyong Yang, Mingli Xiang, Linli Li
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Triptolide-based cleavable antibody-drug conjugates for pancreatic cancer Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-05-29 Huihui Wang, Shangwei Huangfu, Ding Wei, Ziyu Sun, Yifan Wu, Xianqiang Yu, Biao Jiang, Hongli Chen
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Development of a potent BET inhibitor for the treatment of renal fibrosis Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-05-28 Jianhang Huang, Na Zhao, Jian Li, Jiayi Zhu, Guoao Liang, Xing Chen, Naiyuan Wang, Huilong Zhu, Ningning Pang, Chunmei An, Xiaochun Xiong
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Discovery of a potent, broad-spectrum and in vivo effective deuterated tetrazole CYP51 inhibitor Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-05-28 Zirui Luo, Rongrong Liu, Yixiang Sun, Leimeng Zhao, Jiachen Zhang, Kejian Li, Zixuan Gao, Nian Liu, Haoyu Zhang, Xudong Wu, Jingming Liu, Wenzhan Hao, Xin Su, Dongmei Zhao, Maosheng Cheng
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Discovery of new celastrol derivatives with antitumor activity in vitro and invivo by blocking Hsp90-Cdc37-kinase cycle Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-05-28 Lulu Zhang, Jianbo Sun, Junjie Wang, Yue Wang, Wei Ju, Yongqing Zhang, Na Li, Li Chen
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Docking for Smoothened antagonist chemotypes not susceptible to a vismodegib-resistance mutation Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-05-27 Willem H.C. Titulaer, Sebastian Klindert, Corey Taylor, Rebekka A. Schwab, Christian Siebold, Peter Kolb
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Discovery of novel genipin derivatives as highly selective ferroptosis inducers for the treatment of triple-negative breast cancer Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-05-27 Jing-Wen Yu, Yan Cao, Ya-Zheng Zhu, Zheng-Yu Hu, Qing-Jia Ren, Hui Miao, Yong Yin, Cao-Long Li
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The impact of wingtip N-substitution on the bioactivity of azolium salts Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-05-27 Halliru Ibrahim, Muhammad D. Bala, Pinkie Ntola
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Molecular hybridization strategy - discovery of 2,3-diarylpyrazine derivatives as potent Skp2 inhibitors with improved anti-tumor activity and enhanced cisplatin sensitivity Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-05-27 Kaizhao Hu, Kun Zhang, Ruihao Chui, Wenhui Qiu, Peipei Miao, Linlin Zhang, Mengying Ding, Qingjin Zhang, Bing Zhao, Xiao-Jing Shi, Hong-Min Liu
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How generative Artificial Intelligence can transform drug discovery? Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-05-27 Ainin Sofia Jusoh, Muhammad Akmal Remli, Mohd Saberi Mohamad, Tristan Cazenave, Chin Siok Fong
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An overview of isatin-derived CDK2 inhibitors in developing anticancer agents Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-05-27 Mahsa Ansari, Morteza Ghandadi, Saeed Emami
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Indotropane Pseudo-Natural product is a novel class of potent and selective antibacterial agent against methicillin- and vancomycin-resistant S. aureus Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-05-25 Gautam Kumar, Abdul Akhir, Aswin T. Srivatsav, Deepanshi Saxena, Rahul Maitra, Deepak Datta Gaonkar, Shobhna Kapoor, Sidharth Chopra, Rishikesh Narayan
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Exploiting acylaminopyrazole scaffold for polypharmacology approach in Alzheimer's disease Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-05-25 Rebecca Orioli, Giuliana Sarno, Francesca Seghetti, Silvia Gobbi, Federica Belluti, Alessandra Feoli, Francesca Massenzio, Barbara Monti, Rosaria Spagnuolo, Manuela Bartolini, Sabrina Castellano, Alessandra Bisi
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Research progress of ATR small molecule inhibitors in cancer therapy Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-05-24 Shujin Guo, Qiumei He, Yuping Liu, Aili Zou, Yang Liao, Li Guo, Lan Bai, Jianyou Shi
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Design, synthesis and evaluation of anticancer and antioxidant properties of phenolic derivatives incorporating 4H-pyran/1,4-dihydropyridine/1,3-dihydropyrimidinone scaffolds Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-05-23 Selsabil Djafarou, Elen Alves, Imene Amine Khodja, Gökçe Seyhan, Burak Barut, Dominique Harakat, Arif Mermer, David M. Pereira, Houssem Boulebd
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Insights into PTP1B inhibitors as antidiabetic agents: Current research and future perspectives Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-05-23 Abu Sahban Haider, Ramesh Ambatwar, Gopal L. Khatik
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Recent research frontiers of heterocycles as antifungal Agents: Insights from the past five years Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-05-23 Sumit Tahlan, Sucheta Singh, Hrithik Dey, Meenakshi Kaira, Kailash C. Pandey
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Discovery of novel and selective GPR17 antagonists as pharmacological tools for developing new therapeutic strategies in diabetes and obesity Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-05-22 Hu Zhu, Jason M. Conley, Surendra Karavadhi, Justin E. LaVigne, Val J. Watts, Hongmao Sun, Min Shen, Matthew D. Hall, Hongxia Ren, Samarjit Patnaik
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Design, synthesis and structure-activity relationships of novel HIV capsid inhibitors with potent antiviral activities Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-05-22 Dazhou Shi, Shujing Xu, Lin Sun, Prem Prakash Sharma, Brijesh Rathi, Mei Wang, Linan Wu, Xiangyi Jiang, Erik De Clercq, Christophe Pannecouque, Xinyong Liu, Alexej Dick, Peng Zhan
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Design, synthesis and biological evaluation of the activity-based probes for FGFR covalent inhibitor Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-05-22 Dandan Zhu, Zijian Zheng, Huixin Huang, Xiaojuan Chen, Shuhong Zhang, Zhuchu Chen, Ting Liu, Guangyu Xu, Ying Fu, Yongheng Chen
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Design, synthesis, and biological evaluation of indazole-based histone deacetylase 6 inhibitors Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-05-22 Khan Hashim Ali, Sunil K. Gupta, Yong Jin Oh, Mosharof Hossain, Ji Hyun Kim, Sun You Park, Young Ho Seo
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Discovery of novel non-sulfonylurea NLRP3 inflammasome inhibitors for the treatment of multiple inflammatory diseases Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-05-22 Qi Lv, Yuze Wu, Zhiqi Yan, Ying Xie, Zhenzhen Zhu, Wen Xiao, Lihao Zhang, Jian Liu, Junwei Wang, Lihong Hu
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Investigation into the binding domains of platelet factor 4 unlocks new avenues for the design and synthesis of selective sulfated pseudo-tetrasaccharide aminoglycoside ligands Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-05-21 Livia Philip, Hawau Abdulsalam, Kartikey Singh, Hien M. Nguyen
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Successive structural optimization of Ziritaxestat culminates in the discovery of orally bioavailable and in vivo potent imidazothiadiazole derivative for treating ATX-driven diseases Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-05-21 Henian Wang, Yulei Liu, Qinlong Xu, Gaofeng Lin, Li Shao, Jiajia Mo, Jiaming Li, Zhaoxing Chu, Xiaodong Ma
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Corrigendum to “Refinement of imidazo[2,1-a]pyrimidines in pursuit of potential drug candidates against group 2 influenza A viruses” [Europ. J. Med. Chem. 2925 (2025) 117679] Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-05-21 Malaika D. Argade, Varada Anirudhan, Sean P. Bradley, Łukasz Tomorowicz, Ryan Bott, Boopathi Sownthirarajan, Christian A. Zielinski, John P. Sloan, Dejan S. Nikolic, Arsen M. Gaisin, Terry W. Moore, Balaji Manicassamy, Norton P. Peet, Lijun Rong, Irina N. Gaisina
The authors regret that the post-publication review showed the presence of " = " signs before and in some cases after the text in Tables. 1 and 2 (column 3) pasted incorrectly, which was caused by the mismatch of file versions during the revision process. Corrected Tables. 1 and 2 are shown below. Table 1. Chemical structures and anti-influenza activity of imidazo[1,2-a]pyrimidines 1–35. Compound Type
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Characterization of a dual degrader of MDM2 and GSPT1 Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-05-21 Ira Tandon, Paulina N. Esguerra, Chunrong Li, Huan Sun, Ka Yang, Zhongrui Zhang, Junmin Peng, Weiping Tang
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Investigating the structure-activity-relationship of diaryl ether-based paFabV inhibitors: A path to novel antibacterials Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-05-21 Radu-George Bulai, Wout Van Eynde, Sofie Heylen, Maria Cremonini, Flore Van Olmen, Renata Wicik, Eveline Lescrinier, Jef Rozenski, Arnout Voet, Joleen Masschelein, Peter Verwilst
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Discovery of novel diarypyrimidine derivatives as potent HIV-1 NNRTIs by exploiting the tolerant region I within NNRTI binding pocket Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-05-20 Xiangkai Ji, Xiangyi Jiang, Zhen Gao, Heng Gao, Erik De Clercq, Christophe Pannecouque, Dongwei Kang, Peng Zhan, Xinyong Liu
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Temperature vaulting: A method for screening of slow- and tight-binding inhibitors that selectively target kinases in their non-native state Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-05-20 Sora Suzuki, Koji Umezawa, Gaku Furuie, Masaki Kikuchi, Daichi G.M. Nakamura, Nanae Fukahori, Ninako Kimura, Masato Yamakawa, Takashi Niwa, Takashi Umehara, Takamitsu Hosoya, Isao Kii
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Nicotinamide N-methyltransferase in cardiovascular Diseases: Mechanistic insights and therapeutic potential Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-05-20 Shuang-Zhou Bi, Wei-Dong Sun, Xiao-Juan Zhu, Shi-Yan Lai, An-Liu, Chen-Ying Zhang, Jiang-Hua Li
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Genome mining, synthesis, antibacterial mechanism, and application of the gut commensal-derived antibacterial peptide CR24 Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-05-19 Ke Ma, Wei Ran, Xin-long Chu, Jian-gang Zhang, Lei Fu, Peng-cheng Gao, Xue-rui Li, Fei-jie Zhi, Yin-juan Song, Yong-jun Yang, Yue-feng Chu
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New drugs approved by European medicines agency during 2024 Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-05-19 Rong Hu, Dan Liu, Xiaofei Sun, Zhong Yu
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