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Design and evaluation of novel oxadiazole derivatives as potential prostate cancer agents.

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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Mochona B,Qi X,Euynni S,Sikazwi D,Mateeva N,Soliman KF

doi

10.1016/j.bmcl.2016.04.058

subject

Has Abstract

pub_date

2016-06-15 00:00:00

pages

2847-2851

issue

12

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(16)30434-6

journal_volume

26

pub_type

杂志文章

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