| Literature DB >> 27156770 |
Bereket Mochona1, Xin Qi2, Suresh Euynni3, Donald Sikazwi4, Nelly Mateeva1, Karam F Soliman3.
Abstract
Various 1,3,4-oxadiazole derivatives have been synthesized and their antiproliferative properties have been studied. The in vitro screening was performed against androgen dependent (LNCaP) and androgen independent (PC-3) prostate cancer cell lines. Most of the compounds showed promising activity. Among them, compounds 2d (IC50=0.22 and 1.3μM) and 2a (IC50=8.34 and 2,5μM) have shown significant activities on PC-3 and LNCaP cell lines respectively. To investigate the mechanism of cell death we performed cell apoptosis staining and cell cycle arrest assay on more sensitive PC-3 cell lines on 2d. The results demonstrated that 2d induced apoptosis and shifted the cells to the sub G0/G1 and S phase. Our study evidently identified the potency of compound 2d as potential anti-prostate cancer agent. Published by Elsevier Ltd.Entities:
Keywords: 1,3,4-Oxadiazole; Apoptosis; Azoles; Cell cycle; Prostate cancer
Mesh：
Substances：
Year: 2016 PMID： 27156770 PMCID： PMC4888807 DOI： 10.1016/j.bmcl.2016.04.058
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823