Synthesis, antitumor activity evaluation and mechanistic study of novel hederacolchiside A1 derivatives bearing an aryl triazole moiety
Synthesis, antitumor activity evaluation and mechanistic study of novel hederacolchiside A1 derivatives bearing an aryl triazole moiety
复制标题
新型芳基三唑常春藤苷A1衍生物的合成、抗肿瘤活性评价及机理研究
DOI：
10.1016/j.bmc.2018.06.026
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发表时间：
2018-08-07
影响因子：
3.5
通讯作者：
Cheng, Mao-sheng
中科院分区：
文献类型：
--
作者：
Li, Hui-ning;Wang, Hui;Cheng, Mao-sheng
In an attempt to arrive at a more potent antitumor agent than the parent natural saponin hederacolchiside A(1), 23 hederacolchiside A(1) derivatives (4a-4w) were synthesized via Cu(I)-catalyzed azide-alkyne 1,3-dipolar cycloaddition and screened in vitro for cytotoxicity against six human cancer cell lines. The structure-activity relationship of these compounds was elucidated, and the biological screening results showed that most of the compounds exhibited moderate to high levels of antitumor activities against the tested cell lines and some of them displayed more potent inhibitory activities compared with hederacolchiside A(1). Compound 4f showed a 2-to 7-fold more potent activity than hederacolchiside A(1). The mechanistic study of 4f revealed that this compound can induce cell apoptosis in HepG2 cells via mitochondrial-mediated intrinsic pathways.
