Synthesis and biological evaluation of novel 1,2,3-triazole hybrids of cabotegravir: identification of potent antitumor activity against lung cancer

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成果类型：

期刊论文

作者：

Guo, Yajie;Sang, Dan;Guo, Bin;Wang, Dan;Xu, Xinyue;...

通讯作者：

Hou, CL;Mao, Longfei;Li, SQ;Mao, LF;Li, F

作者机构：

[Guo, Yajie] Sun Yat Sen Univ, Affiliated Hosp 8, Dept Emergency, Shenzhen, Peoples R China.

[Sang, Dan] Sun Yat Sen Univ, Affiliated Hosp 8, Dept Endocrinol, Shenzhen, Peoples R China.

[Guo, Bin] Univ Sci & Technol China, Affiliated Hosp 1, Ultrason Dept, Div Life Sci & Med, Hefei, Anhui, Peoples R China.

[Wang, Dan] Southern Med Univ, Sch Publ Hlth, Guangzhou, Peoples R China.

[Wang, Dan; Xu, Xinyue] Shenzhen Ctr Dis Control & Prevent, Shenzhen, Peoples R China.

通讯机构：

[Li, SQ ; Li, F ; Mao, LF] H

[Mao, LF ] N

[Hou, CL ] S

Shanghai Jiao Tong Univ, Shanghai Childrens Hosp, Dept Cardiol, Shanghai, Peoples R China.

Henan Univ Sci & Technol, Coll Basic Med & Forens Med, Luoyang, Peoples R China.

语种：

英文

关键词：

1,2,3-triazoles;ROS;anticancer;apoptosis;cabotegravir;lung cancer

期刊：

Frontiers in Pharmacology

ISSN：

1663-9812

年：

2023

卷：

页码：

1265245

DOI：

10.3389/fphar.2023.1265245

基金类别：

The author(s) declare financial support was received for the research, authorship, and/or publication of this article. This work was supported by National Natural Science Foundation of China (82170606), Basic Research Project of Key Scientific Research Projects of Universities in Henan Province (23ZX006), Shenzhen Science and Technology Program (No. JCYJ20210324115208024), Shenzhen Outbound Postdoctoral Research Grant (No.CZBSHKYJJ002).

机构署名：

本校为其他机构

院系归属：

公共卫生学院

摘要：

In pursuit of discovering novel anticancer agents, we designed and synthesized a series of novel 1,2,3-triazole hybrids based on cabotegravir analogues. These compounds were subjected to initial biological evaluations to assess their anticancer activities against non-small-cell lung cancer (NSCLC). Our findings indicated that some of these compounds exhibited promising antitumor abilities against H460 cells, while demonstrated less efficacy against H1299 cells. Notably, compound 5i emerged as the most potent, displaying an IC50 value of 6.06μM...

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Synthesis and biological evaluation of novel 1,2,3-triazole hybrids of cabotegravir: identification of potent antitumor activity against lung cancer

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