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Design and Synthesis of Novel Dehydroepiandrosterone Analogues as Potent Antiproliferative Agents

Authors :
Xing Huang
Qing-Kun Shen
Hong-Jian Zhang
Jia-Li Li
Yu-Shun Tian
Zhe-Shan Quan
Source :
Molecules, Vol 23, Iss 9, p 2243 (2018)
Publication Year :
2018
Publisher :
MDPI AG, 2018.

Abstract

The aim of the present study was to determine the cytotoxic effects of a series of novel dehydroepiandrosterone derivatives containing triazole at the C16 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 µM, and considerably high activity against the MCF-7 cell line, with an IC50 value of 9.18 µM. Flow cytometry assays demonstrated that compound 2n exerted antiproliferative effects by arresting cells in the G2 phase of the cell cycle and inducing apoptosis.

Details

Language :
English
ISSN :
14203049
Volume :
23
Issue :
9
Database :
Directory of Open Access Journals
Journal :
Molecules
Publication Type :
Academic Journal
Accession number :
edsdoj.3c45eca829ce4e2c9f1cee13313e582b
Document Type :
article
Full Text :
https://doi.org/10.3390/molecules23092243