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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 1.3?M) and 2a (IC50=8.34 and 2,5?M) 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.

SUBMITTER: Mochona B

PROVIDER: S-EPMC4888807 | biostudies-literature | 2016 Jun

REPOSITORIES: biostudies-literature

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

Mochona Bereket B Qi Xin X Euynni Suresh S Sikazwi Donald D Mateeva Nelly N Soliman Karam F KF

Bioorganic & medicinal chemistry letters 20160421 12

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 per ...[more]

PMID: 27156770

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