Novel ester tethered dihydroartemisinin-3-(oxime/thiosemicarbazide)isatin hybrids as potential anti-breast cancer agents: Synthesis, in vitro cytotoxicity and structure-activity relationship

被引：2
|
作者：
Liu, Shaohuan [1 ,2 ]
Wang, Shu [1 ]
Xu, Dan [3 ]
Pan, Bowen [3 ]
Chen, Linzhi [3 ]
Zhao, Shijia [2 ]
Xu, Zhi [3 ]
Zhou, Wei [2 ]
机构：
[1] Sichuan Univ, West China Sch Pharm, Chengdu, Sichuan Provinc, Peoples R China
[2] Guizhou Med Univ, Sch Pharm, Guiyang, Guizhou, Peoples R China
[3] Guizhou Univ Tradit Chinese Med, Sch Pharm, Guiyang, Guizhou, Peoples R China
来源：
DRUG DEVELOPMENT RESEARCH | 2023年 / 84卷 / 06期
关键词：
breast cancer; dihydroartemisinin; isatin; structure-activity relationship; thiosemicarbazide; DIHYDROARTEMISININ; HYDROGEN;
D O I：
10.1002/ddr.22078
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of ester tethered dihydroartemisinin-3-(oxime/thiosemicarbazide)isatin hybrids 7a-p were designed, synthesized, and assessed for their antiproliferative activity against MCF-7, MDA-MB-231, MCF-7/ADR, and MDA-MB-231/ADR breast cancer cell lines. Among them, hybrids 7a,f (IC50: 1.33-3.84 mu M) showed potent activity against triple-negative (MDA-MB-231 and MDA-MB-231/ADR) breast cancer cell lines, and hybrid 7f (IC50: 3.90 and 10.18 mu M) also demonstrated promising activity against estrogen receptor-positive breast cancer cells (MCF-7 and MCF-7/ADR), and the activity was superior to these of artemisinin, dihydroartemisinin, and ADR, revealing their potential to fight against both drug-sensitive and drug-resistant breast cancers. The enriched structure-activity relationships may facilitate further design of more active candidates.
引用
收藏
页码：1175 / 1182
页数：8
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