European Journal of Medicinal Chemistry

Design, synthesis, ADME and biological evaluation of benzylpiperidine and benzylpiperazine derivatives as novel reversible monoacylglycerol lipase (MAGL) inhibitors

Publication date: Available online 2 November 2023Source: European Journal of Medicinal ChemistryAuthor(s): Miriana Di Stefano, Samuele Masoni, Giulia Bononi, Giulio Poli, Salvatore Galati, Francesca Gado, Simone Manzi, Chiara Vagaggini, Annalaura Brai…

By ScienceDirect Publication: European Journal of Medicinal Chemistry, ago

Discovery of (<em>R</em>)-4-(8-methoxy-2-methyl-1-(1-phenylethy)-1<em>H</em>-imidazo[4,5-<em>c</em>]quinnolin-7-yl)-3,5-dimethylisoxazole as a potent and selective BET inhibitor for treatment of acute myeloid leukemia (AML) guided by FEP calculation

Publication date: Available online 7 November 2023Source: European Journal of Medicinal ChemistryAuthor(s): Su Yu, Yan Zhang, Jie Yang, Hongrui Xu, Suke Lan, Binyan Zhao, Meng Luo, Xinyu Ma, Hongjia Zhang, Shirui Wang, Hui Shen, Yan Zhang, Yong Xu, Rui Li

By ScienceDirect Publication: European Journal of Medicinal Chemistry, ago

A novel scaffold long-acting selective estrogen receptor antagonist and degrader with superior preclinical profile against ER+ breast cancer

Publication date: Available online 8 November 2023Source: European Journal of Medicinal ChemistryAuthor(s): Bingsi Wang, Mingxu Ma, Yusen Dai, Pengfei Yu, Liang Ye, Wenyan Wang, Chunjie Sha, Huijie Yang, Yingjie Yang, Yunjing Zhu, Lin Dong, Shujuan Wei…

By ScienceDirect Publication: European Journal of Medicinal Chemistry, ago

5-(Trifluoromethyl)-1,2,4-oxadiazole (TFMO)-based highly selective class IIa HDAC inhibitors exhibit synergistic anticancer activity in combination with bortezomib

Publication date: Available online 10 November 2023Source: European Journal of Medicinal ChemistryAuthor(s): Yodita Asfaha, Lukas M. Bollmann, Alexander J. Skerhut, Fabian Fischer, Nadine Horstick, Dennis Roth, Maria Wecker, Christian Mammen, Sander H….

By ScienceDirect Publication: European Journal of Medicinal Chemistry, ago

Development of a new class of potent and highly selective G protein-coupled receptor kinase 5 inhibitors and structural insight from crystal structures of inhibitor complexes

Publication date: Available online 10 November 2023Source: European Journal of Medicinal ChemistryAuthor(s): Yueyi Chen, Amol Sonawane, Rajesh Manda, Ranjith Kumar Gadi, John J.G. Tesmer, Arun K. Ghosh

By ScienceDirect Publication: European Journal of Medicinal Chemistry, ago