title: Design, synthesis and biological evaluation of novel arylpiperazine derivatives on human prostate cancer cell lines.
abstract: A series of novel arylpiperazine derivatives was synthesized. The in vitro cytotoxic activities of all synthesized compounds against three human prostate cancer cell lines (PC-3, LNCaP, and DU145) were evaluated by a CCK-8 assay. Compounds 10, 24 and 29 exhibited strong cytotoxic activities against LNCaP cells (IC50 <3μM). In addition, these compounds exhibited weak cytotoxic effects on human epithelial prostate normal cells RWPE-1. The structure-activity relationship (SAR) of these arylpiperazine derivatives was also discussed based on the obtained experimental data.
authors.affiliation: Pharmaceutical Research Center, Guangzhou Medical University, Guangzhou 510182, China.
authors.forename: Hong
authors.initials: H
authors.lastname: Chen
authors.affiliation: Pharmaceutical Research Center, Guangzhou Medical University, Guangzhou 510182, China.
authors.forename: Fang
authors.initials: F
authors.lastname: Xu
authors.affiliation: Pharmaceutical Research Center, Guangzhou Medical University, Guangzhou 510182, China.
authors.forename: Xue
authors.initials: X
authors.lastname: Liang
authors.affiliation: Pharmaceutical Research Center, Guangzhou Medical University, Guangzhou 510182, China.
authors.forename: Bing-Bing
authors.initials: BB
authors.lastname: Xu
authors.affiliation: Pharmaceutical Research Center, Guangzhou Medical University, Guangzhou 510182, China.
authors.forename: Zong-Lin
authors.initials: ZL
authors.lastname: Yang
authors.affiliation: Pharmaceutical Research Center, Guangzhou Medical University, Guangzhou 510182, China.
authors.forename: Xue-Lan
authors.initials: XL
authors.lastname: He
authors.affiliation: Pharmaceutical Research Center, Guangzhou Medical University, Guangzhou 510182, China.
authors.forename: Bi-Yun
authors.initials: BY
authors.lastname: Huang
authors.affiliation: Pharmaceutical Research Center, Guangzhou Medical University, Guangzhou 510182, China. Electronic address: mryuanmu838@sina.com.
authors.forename: Mu
authors.initials: M
authors.lastname: Yuan
mesh_terms: D000970:Antineoplastic Agents / Q000494:pharmacology*; D049109:Cell Proliferation / Q000187:drug effects*; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D008297:Male; D008958:Models, Molecular; D015394:Molecular Structure; D010879:Piperazines / Q000138:chemical synthesis* / Q000494:pharmacology*; D011471:Prostatic Neoplasms / Q000188:drug therapy* / Q000473:pathology; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
chemical_list: D000970:Antineoplastic Agents; D010879:Piperazines
keywords: Arylpiperazine derivatives; CCK-8; Cytotoxic activity; Structure–activity relationship; Synthesis