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.
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页数：14
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