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含1,2,3-三唑的卡博特韦衍生物的设计与合成及抗肝癌活性评价

Design and synthesis of cabotegravir derivatives bearing 1,2,3-triazole and evaluation of anti-liver cancer activity.

作者信息

Xie Huaxia, Mao Longfei, Fan Gaolu, Wu Ziyuan, Wang Yimian, Hou Xixi, Wang Jiangang, Wang Huili, Liu Ling, Li Sanqiang

机构信息

College of Basic Medicine and Forensic Medicine, Henan University of Science and Technology, Luoyang, China.

Department of Pharmacy, Luoyang Third People's Hospital, Luoyang, China.

出版信息

Front Pharmacol. 2023 Oct 6;14:1265289. doi: 10.3389/fphar.2023.1265289. eCollection 2023.

DOI:10.3389/fphar.2023.1265289
PMID:37869757
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10590056/
Abstract

Based on the structure of the anti-HIV drug cabotegravir, we introduced 1,2,3-triazole groups with different substituents to obtain 19 cabotegravir derivatives and tested their activity against HepG2 cells. The proliferation of HepG2 cells was examined following treatment with derivatives. Most of the compounds demonstrated significant inhibitory effects, particularly compounds KJ-5 and KJ-12 with IC values of 4.29 ± 0.10 and 4.07 ± 0.09 μM, respectively. Furthermore, both compounds 5 and 12 significantly caused cell apoptosis, G2/M arrest, and DNA damage, and suppressed invasion and migration in a concentration-dependent manner. In addition, KJ-5 and KJ-12 could trigger apoptosis via the mitochondrial pathway by increasing the ratio of Bax/Bcl-2 and activating cleaved caspase-9, cleaved caspase-3, and cleaved PARP.

摘要

基于抗HIV药物卡博特韦的结构，我们引入了带有不同取代基的1,2,3-三唑基团，以获得19种卡博特韦衍生物，并测试了它们对HepG2细胞的活性。在用衍生物处理后检测HepG2细胞的增殖情况。大多数化合物表现出显著的抑制作用，尤其是化合物KJ-5和KJ-12，其IC值分别为4.29±0.10和4.07±0.09μM。此外，化合物5和12均显著引起细胞凋亡、G2/M期阻滞和DNA损伤，并以浓度依赖的方式抑制侵袭和迁移。此外，KJ-5和KJ-12可通过增加Bax/Bcl-2的比值并激活裂解的caspase-9、裂解的caspase-3和裂解的PARP，经由线粒体途径触发细胞凋亡。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f3ae/10590056/61360f92ef6f/fphar-14-1265289-g011.jpg
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