title: Synthesis and cytotoxic activity 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 9 and 15 exhibited strong cytotoxic activities against LNCaP cells (IC50<5 μM), and compound 8 (IC50=8.25 μM) possessed the most potent activity against DU145 cells. However, these compounds also exhibited cytotoxicity towards 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, 195# Dongfengxi Road, Guangzhou 510182, China. chenwexpo@sina.com.
authors.forename: Hong
authors.initials: H
authors.lastname: Chen
authors.affiliation: Pharmaceutical Research Center, Guangzhou Medical University, 195# Dongfengxi Road, Guangzhou 510182, China. liangliang4983@163.com.
authors.forename: Xue
authors.initials: X
authors.lastname: Liang
authors.affiliation: Pharmaceutical Research Center, Guangzhou Medical University, 195# Dongfengxi Road, Guangzhou 510182, China. sherrywon03@163.com.
authors.forename: Fang
authors.initials: F
authors.lastname: Xu
authors.affiliation: Pharmaceutical Research Center, Guangzhou Medical University, 195# Dongfengxi Road, Guangzhou 510182, China. yjxubb@163.com.
authors.forename: Bingbing
authors.initials: B
authors.lastname: Xu
authors.affiliation: Pharmaceutical Research Center, Guangzhou Medical University, 195# Dongfengxi Road, Guangzhou 510182, China. gzmc_xlhe@hotmail.com.
authors.forename: Xuelan
authors.initials: X
authors.lastname: He
authors.affiliation: Pharmaceutical Research Center, Guangzhou Medical University, 195# Dongfengxi Road, Guangzhou 510182, China. guangyihby@126.com.
authors.forename: Biyun
authors.initials: B
authors.lastname: Huang
authors.affiliation: Pharmaceutical Research Center, Guangzhou Medical University, 195# Dongfengxi Road, Guangzhou 510182, China. mryuanmu838@sina.com.
authors.forename: Mu
authors.initials: M
authors.lastname: Yuan
mesh_terms: D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D008297:Male; D000077489:Piperazine; D010879:Piperazines / Q000008:administration & dosage* / Q000138:chemical synthesis* / Q000737:chemistry; D011471:Prostatic Neoplasms / Q000188:drug therapy* / Q000473:pathology; D013329:Structure-Activity Relationship
chemical_list: D010879:Piperazines; D000077489:Piperazine