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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 -
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 -
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 -
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 -
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 -
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 -
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 -
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 -
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 -
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, Alexander.F. Kiefer, Jörg Haupenthal, Ansgar Dellmann, Duc.T. Huynh, Ruoyu Zhang, Wulf Blankenfeldt, Anna.K.H. Hirsch, Michael Steinert -
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 -
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 -
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 -
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 -
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 -
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 -
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 -
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 -
Discovery of new celastrol derivatives with antitumor activity in vitro and in vivo 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 -
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 -
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 -
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 -
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 -
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 -
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 -
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 -
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 -
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 -
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 -
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 -
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 -
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 -
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 -
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 -
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 -
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 -
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 -
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. GaisinaThe 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 -
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 -
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 -
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 -
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 -
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 -
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 -
In pursuit of cytotoxic triterpenoids. Functionalization of lupane, taraxastane, friedelane, and baccharane derivatives via oxidation with selenium reagents Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-05-19
Kinga Kuczynska, Piotr Cmoch, Lucie Rárová, Jarosław Jaźwiński, Anna Korda, Jacek W. Morzycki, Marie Kvasnicová, Katarzyna Gwardiak, Romuald Karczewski, Mohadese Yaghoobi Anzabi, Roman Luboradzki, Miroslav Strnad, Zbigniew Pakulski -
Reversing an agonist into an inhibitor: Development of mTOR degraders Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-05-17
Liquan Zhu, Siyi Fu, Longfei Ma, Zhe Chen, Qian Zeng, Ruichen Li, Yiyu Zhou, Huijuan Qian, Xuli Meng, Jingyan Ge -
Design and synthesis of CDK9/EZH2 dual-target inhibitors to achieve synergistic antitumor effects Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-05-17
Lina Tian, Jian Xiao, Yanping Zeng, Yangsha Li, Aihuan Wei, Qianqian Shen, Yixue Han, Yi Chen, Youhong Hu -
Discovery of potent anti-idiopathic pulmonary fibrosis (IPF) agents based on an o-aminopyridinyl alkynyl scaffold Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-05-16
Yang Wang, Wenhui Fan, Yihao Guo, Li Sun, Youhong Hu, Jing Chen, Likun Gong, Zhicheng Xie -
Chromanone derivatives: Evaluating selective anticancer activity across human cell lines Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-05-16
Marta Sobiesiak, Nadia Fatyga, Aleksander Brzozowski, Adam Sikora, Bogumiła Kupcewicz, Małgorzata Maj -
D-Alanine functionalized Iridium(III) complexes as two-photon photo-antibiotics for bacteria-specific ablation in infected macrophages Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-05-15
Jun Shu, Hui Jiang, Minwei Lin, Jinzhe Liang, Yukun Zhao, Diqing Luo, Jinquan Wang, Hui Chao -
Discovery of a potent and selective peptide inhibitor with d-amino acids targeting the BRD4 ET domain for renal cancer therapy Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-05-15
Nan Jiang, Mengting Lou, Nan Wu, Yifei Geng, Miao-Miao Niu, Yang Zhou, Shizhu Zhang -
Probing new 3-hydrazinyl indole phenacetamide derivatives as multitarget anti-Alzheimer: Synthesis, in vivo, in vitro, and in silico studies Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-05-15
Mona F. Said, Walaa Wadie, Enas A. Abd El-Haleim, Riham A. El Shiekh, Haidy H. El-Zoheiry -
Ellipticine derivatives as Toll-like receptor 3 inhibitor for treating acute hepatitis Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-05-14
Zhuoxian Cao, Meixin Liu, Mingze Yang, Xiao Li, Xiaoxiao Xia, Kui Cheng -
Design, synthesis, and biological evaluation of C-12 modified ocotillol-type derivatives as novel P-glycoprotein modulators for overcoming multidrug resistance Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-05-14
Cheng Chen, Ziqian Hao, Jiaxuan Chen, Shuang Li, Yongyuan Su, Suwei Jiang, Lin Ma, Hanqi Lv, Xinjie Pei, Peng Zhang, Hongbo Wang, Gangqiang Yang -
Approaching Gallium-68 radiopharmaceuticals for tumor diagnosis: a Medicinal Chemist's perspective Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-05-14
Francesca Musumeci, Alessandro Fasce, Marta Falesiedi, Federica Oleari, Giancarlo Grossi, Anna Carbone, Silvia Schenone -
Advances in fluorescent natural products for imaging localization and biological applications Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-05-14
Guiqian Fang, Daili Liu, Yuanzhuo Wang, Qingqiang Yao -
Design, synthesis, and biological evaluation of TRPV4-KCa2.3 coupling enhancers as novel therapeutic agents for hypertension Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-05-13
Shaying Yang, Dongyu Wang, Huabing Wang, Junlan Shao, Chunlei Tang -
Structure-directing optimization of N-(2,3-dihydrobenzo[b] [1,4]dioxin-6-yl)benzamide derivatives as selective receptor tyrosine kinase-like orphan receptor 1 (ROR1) inhibitors for cancer therapy Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-05-13
Qingquan Zheng, Hulin Ma, Dongdong Luo, Xingyang Qiu, Yue Ming, Wenchen Pu, Min Ai, Jianhua He, Yong Peng -
Discovery of N-(3-fluorophenyl)-2-(4-((7-(1-methyl-1H-pyrazol-4-yl)quinazolin-4-yl)amino)phenyl)acetamide as the first orally active selective aurora kinase B inhibitor Eur. J. Med. Chem. (IF 6.0) Pub Date : 2025-05-13
Phuc Tran, Marialuisa Moccia, Xiuqi Wang, Annalisa Brescia, Giorgia Federico, Naresh Gunaganti, Zhengyu Wang, Min Yang, Minmin Wang, Baha'a Jabali, Wei Yan, Brendan Frett, Massimo Santoro, Francesca Carlomagno, Hong-yu Li