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Synthesis and discovery of novel 1,2,3-triazole based cabotegravir derivatives with potent anticancer activity

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成果类型:
期刊论文
作者:
Guo, Yajie;Hou, Jingyu;Wu, Hao;Chen, Ying;Liu, Guangnan;...
通讯作者:
Wang, T;Mao, Longfei;Li, SQ
作者机构:
[Guo, Yajie; Wang, Tong; Wang, T; Hou, Jingyu] Sun Yat Sen Univ, Affiliated Hosp 8, Dept Emergency, Shenzhen 518033, Peoples R China.
[Wu, Hao] Sun Yat sen Univ, Sun Yat Sen Mem Hosp, Dept Emergency, Guangzhou 510120, Peoples R China.
[Chen, Ying; Liu, Guangnan] Univ South China, Sch Publ Hlth, Hengyang 421000, Peoples R China.
[Chen, Ying; Liu, Guangnan] Shenzhen Ctr Dis Control & Prevent, Shenzhen 518055, Peoples R China.
[Wang, Dan] Southern Med Univ, Sch Publ Hlth, Guangzhou 510515, Peoples R China.
通讯机构:
[Li, SQ ; Mao, LF] H
[Wang, T ] S
Sun Yat Sen Univ, Affiliated Hosp 8, Dept Emergency, Shenzhen 518033, Peoples R China.
Henan Univ Sci & Technol, Coll Basic Med & Forens Med, Luoyang 471003, Peoples R China.
语种:
英文
关键词:
1,2,3-Triazole;Cabotegravir;Anti-cancer
期刊:
Journal of Molecular Structure
ISSN:
0022-2860
年:
2024
卷:
1298
页码:
137042
基金类别:
This work was supported by National Natural Science Foundation of China (NO. 82170606, 81070125, 81270213, 81670306), Basic Research Project of Key Scientific Research Projects of Universities in Henan Province (23ZX006), the Science and Technology Foundation in Guangdong Province (No. 2010B031600032, 2014A020211002), the National Natural Science Foundation of Guangdong Province (No. 2017A030313503), the Science and Technology Foundation in Guangzhou City (No. 201806020084), Shenzhen Science and Technology Program (No. JCYJ20210324115208024, JCYJ20190808101405466, JCYJ20210324115003008, JCYJ20220530144404009), 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:
A series of 28 novel cabotegravir derivatives, incorporating the 1,2,3-triazole moiety, were designed and synthesized. The synthesized compounds were evaluated for their potential anticancer activity against four different human cancer cell lines: HuH-7 (hepatocellular), MCF-7 (breast), SKOV3 (ovarian), and HCT-116 (colon). Initial biological assessments revealed that several compounds exhibited potent anti-proliferative activity against these cancer cell lines. Notably, compounds KJ9 and KJ23 demonstrated the most pronounced effects, with IC50 values of 6.59 and 7.83 mu M in HuH-7 cells, 27.2...

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