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Synthesis, optimization and antitumor activity evaluation of sulfonyl benzoyl hydrazide derivatives as novel human LSD1 inhibitors

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机构： [1]Laboratory of Anaesthesiology & Critical Care Medicine, Department of Anesthesiology, State Key Laboratory of Biotherapy and Cancer Center and Collaborative Innovation Center for Biotherapy, West China Hospital, Sichuan University, Chengdu, Sichuan 610041, China [2]Laboratory of Cardiac Structure and Function, Institute of Cardiovascular Diseases, West China Hospital, Sichuan University, Chengdu, PR China

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关键词： LSD1 Benzoyl hydrazide derivatives Structure–activity relationship

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A new set of compounds known as sulfonyl benzoyl hydrazide derivatives were synthesized and tested using cellular assays. Through systematic optimization starting from general structure S-1, compound 10e emerged as highly promising. It exhibited potent inhibitory activity with an IC50 value of 0.8 nM and possessed moderate clogP. Compounds 10e significantly inhibited solid tumor cells proliferation. Additionally, 10e induced apoptosis and arrested the cell cycle. Furthermore, in vivo studies using an HCT116 xenograft model showed substantial growth inhibition of tumors, accompanied by a favorable safety profile. These findings underscored compound 10e as a novel LSD1 inhibitor with robust efficacy both in vitro and in vivo, establishing it as a promising lead compound for further anticancer drug development.Copyright © 2024 Elsevier Ltd. All rights reserved.

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出版当年[2023]版：

大类 | 4 区医学

小类 | 2 区有机化学 4 区药物化学

最新[2023]版：

大类 | 4 区医学

小类 | 2 区有机化学 4 区药物化学

第一作者：

第一作者机构： [1]Laboratory of Anaesthesiology & Critical Care Medicine, Department of Anesthesiology, State Key Laboratory of Biotherapy and Cancer Center and Collaborative Innovation Center for Biotherapy, West China Hospital, Sichuan University, Chengdu, Sichuan 610041, China

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通讯机构： [1]Laboratory of Anaesthesiology & Critical Care Medicine, Department of Anesthesiology, State Key Laboratory of Biotherapy and Cancer Center and Collaborative Innovation Center for Biotherapy, West China Hospital, Sichuan University, Chengdu, Sichuan 610041, China [2]Laboratory of Cardiac Structure and Function, Institute of Cardiovascular Diseases, West China Hospital, Sichuan University, Chengdu, PR China

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Synthesis, optimization and antitumor activity evaluation of sulfonyl benzoyl hydrazide derivatives as novel human LSD1 inhibitors

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