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

  • Bioorg Med Chem Lett. 2016 Jun 15;26(12):2847-2851. doi: 10.1016/j.bmcl.2016.04.058.
Bereket Mochona  1 ,  Xin Qi  2 ,  Suresh Euynni  3 ,  Donald Sikazwi  4 ,  Nelly Mateeva  1 ,  Karam F Soliman  3
Affiliations
  • 1. Department of Chemistry, Florida A&M University, Tallahassee, FL 32307, United States.
  • 2. Department of Medicinal Chemistry, College of Pharmacy, University of Florida, Gainesville, FL 32603, United States.
  • 3. College of Pharmacy and Pharmaceutical Sciences, Florida A&M University, Tallahassee, FL 32307, United States.
  • 4. Feik School of Pharmacy, University of the Incarnate Word, San Antonio, TX 78209, United States.
PMID: 27156770 DOI: 10.1016/j.bmcl.2016.04.058
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.

Keywords
1,3,4-Oxadiazole; Apoptosis; Azoles; Cell cycle; Prostate cancer.