Design and Synthesis of Novel Dehydroepiandrosterone Analogues as Potent Antiproliferative Agents.

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.

SUBMITTER: Huang X 

PROVIDER: S-EPMC6225165 | biostudies-literature | 2018 Sep

REPOSITORIES: biostudies-literature