Design and Synthesis of Novel Dehydroepiandrosterone Analogues as Potent Antiproliferative Agents

被引：22

作者：

Huang, Xing ^{[1
]}

Shen, Qing-Kun ^{[1
]}

Zhang, Hong-Jian ^{[1
]}

Li, Jia-Li ^{[1
]}

Tian, Yu-Shun ^{[1
]}

Quan, Zhe-Shan ^{[1
]}

机构：

[1] Yanbian Univ, Key Lab Nat Resources & Funct Mol Changbai Mt, Affiliated Minist Educ, Coll Pharm, Yanji 133002, Peoples R China

来源：

MOLECULES | 2018年 / 23卷 / 09期

基金：

中国国家自然科学基金;

关键词：

dehydroepiandrosterone; 1,2,3-Triazoles; antiproliferative; synthesis; IN-VITRO; BIOLOGICAL EVALUATION; DERIVATIVES; ANTIPROTOZOAL; ALPHA; CELLS;

D O I：

10.3390/molecules23092243

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：

The aim of the present study was to determine the cytotoxic effects of a series of novel dehydroepiandrosterone derivatives containing triazole at the C-16 position on human cancer cells. The cancer cells used in the present study were A549, Hela, HepG-2, BEL7402, MCF-7, and HCT116. Several of the synthesised compounds exhibited potent antiproliferative effects. The most promising compound was (E)-3-hydroxy-16-((1-(4-iodophenyl)-1H-1,2,3-triazole-4-yl) methylene)10,13- dimet-hyl-1,3,4,7,8,9,10,11,12,13,15,16-dodecahydro-2H-cyclopenta[a] phenanthren-17(14)-one (compound 2n), which showed considerably high antiproliferative activity in the HepG-2 cell line, with an IC50 value of 9.10 mu M, and considerably high activity against the MCF-7 cell line, with an IC50 value of 9.18 mu M. Flow cytometry assays demonstrated that compound 2n exerted antiproliferative effects by arresting cells in the G2 phase of the cell cycle and inducing apoptosis.

引用

页数：14

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