title: 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.
authors.affiliation: Department of Chemistry, Florida A&M University, Tallahassee, FL 32307, United States.
authors.forename: Bereket
authors.initials: B
authors.lastname: Mochona
authors.affiliation: Department of Medicinal Chemistry, College of Pharmacy, University of Florida, Gainesville, FL 32603, United States.
authors.forename: Xin
authors.initials: X
authors.lastname: Qi
authors.affiliation: College of Pharmacy and Pharmaceutical Sciences, Florida A&M University, Tallahassee, FL 32307, United States.
authors.forename: Suresh
authors.initials: S
authors.lastname: Euynni
authors.affiliation: Feik School of Pharmacy, University of the Incarnate Word, San Antonio, TX 78209, United States.
authors.forename: Donald
authors.initials: D
authors.lastname: Sikazwi
authors.affiliation: Department of Chemistry, Florida A&M University, Tallahassee, FL 32307, United States.
authors.forename: Nelly
authors.initials: N
authors.lastname: Mateeva
authors.affiliation: College of Pharmacy and Pharmaceutical Sciences, Florida A&M University, Tallahassee, FL 32307, United States.
authors.forename: Karam F
authors.initials: KF
authors.lastname: Soliman
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D059447:Cell Cycle Checkpoints / Q000187:drug effects; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D008297:Male; D008958:Models, Molecular; D015394:Molecular Structure; D010069:Oxadiazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D011471:Prostatic Neoplasms / Q000188:drug therapy* / Q000473:pathology; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D010069:Oxadiazoles
keywords: 1,3,4-Oxadiazole; Apoptosis; Azoles; Cell cycle; Prostate cancer