Design, Synthesis, and Antitumor Activity Evaluation of Artemisinin Bivalent Ligands

被引：1

作者：

Zhong, Hui ^{[1
]}

Jiang, Qi ^{[1
]}

Wu, Cong ^{[1
]}

Yu, Huanghe ^{[1
,2
]}

Li, Bin ^{[1
,2
]}

Zhou, Xudong ^{[1
,2
]}

Fu, Ronggeng ^{[1
]}

Wang, Wei ^{[1
,2
]}

Sheng, Wenbing ^{[1
,2
]}

机构：

[1] Hunan Univ Chinese Med, Sch Pharm, Changsha 410208, Peoples R China

[2] Hunan Univ Chinese Med, TCM & Ethnomed Innovat & Dev Int Lab, Changsha 410208, Peoples R China

来源：

MOLECULES | 2024年 / 29卷 / 02期

关键词：

artemisinin; bivalent ligands; multi-target molecular docking; antitumor target protein; antitumor activity; BRIDGED PORPHYRINS; IN-VITRO; CANCER; ANTIMALARIAL; DERIVATIVES; POTENT; DIMERS; BCL-2; MECHANISMS; EXPRESSION;

D O I：

10.3390/molecules29020409

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Five artemisinin bivalent ligands molecules 4a-4e were designed, synthesized, and confirmed by 1H NMR, 13C NMR, and low-resolution mass spectrometry, and the bioactivities of the target compounds were investigated against four human tumor cell lines in vitro, including BGC-823, HepG-2, MCF-7, and HCT-116. The results showed 4a, 4d, and 4e exhibited significantly tumor cell inhibitory activity compared with the artemisinin and dihydroartemisinin; compound 4e has good biological activity inhibiting BGC-823 with an IC50 value of 8.30 mu mol/L. Then, the good correlations with biological results were validated by molecular docking through the established bivalent ligands multi-target model, which showed that 4e could bind well with the antitumor protein MMP-9.

引用

页数：14

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