The design, synthesis and biological evaluation of a novel series of arylpiperazine derivatives of diphenylsulfide with dual 5- HT1A/SSRI activities are reported. The target compounds exhibit low to moderate 5-HT tran...The design, synthesis and biological evaluation of a novel series of arylpiperazine derivatives of diphenylsulfide with dual 5- HT1A/SSRI activities are reported. The target compounds exhibit low to moderate 5-HT transporter affinity and moderate to high 5- HT1A affinity, Compound 13a shows moderate dual activities and is a promising lead compound for further structure-activity relationships studies.展开更多
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, LNCa P, and DU145） were evaluated by ...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, LNCa P, and DU145） were evaluated by a CCK-8 assay. Compounds 8, 10, 13, 17 and 20 exhibited strong cytotoxic activities against the tested cancer cell lines（IC_（50）〈3 μmol/L）. In addition, these compounds exhibited weak cytotoxic effects on human epithelial prostate normal cells WPMY-1. The structure-activity relationship（SAR） of these arylpiperazine derivatives was also discussed based on the obtained experimental data.展开更多
A series of 3-（4-arylpiperazin-1-yl）-1-（benzo[b]thiophen-3-yl）-2-methylpropanol derivatives were designed and synthesized based on 5-HT1A/SSRI drugs design strategies.The synthesized compounds were evaluated for t...A series of 3-（4-arylpiperazin-1-yl）-1-（benzo[b]thiophen-3-yl）-2-methylpropanol derivatives were designed and synthesized based on 5-HT1A/SSRI drugs design strategies.The synthesized compounds were evaluated for their dual 5-HT1A/5-HTT activities.展开更多
文摘The design, synthesis and biological evaluation of a novel series of arylpiperazine derivatives of diphenylsulfide with dual 5- HT1A/SSRI activities are reported. The target compounds exhibit low to moderate 5-HT transporter affinity and moderate to high 5- HT1A affinity, Compound 13a shows moderate dual activities and is a promising lead compound for further structure-activity relationships studies.
基金supported by the Technological Innovation Project of Colleges and Universities in Guangdong Province (No. cx2d1127)the China Postdoctoral Science Foundation (Nos. 2013M542165, 2013M531837)+1 种基金the National Science Foundation of Guangdong Province (No. S2013040014088)the Guangzhou Postdoctoral Scientific Research Foundation (Nos. Q130, Q074)
文摘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, LNCa P, and DU145） were evaluated by a CCK-8 assay. Compounds 8, 10, 13, 17 and 20 exhibited strong cytotoxic activities against the tested cancer cell lines（IC_（50）〈3 μmol/L）. In addition, these compounds exhibited weak cytotoxic effects on human epithelial prostate normal cells WPMY-1. The structure-activity relationship（SAR） of these arylpiperazine derivatives was also discussed based on the obtained experimental data.
基金supported by the National Natural Science Foundation of China(No.20576094).
文摘A series of 3-（4-arylpiperazin-1-yl）-1-（benzo[b]thiophen-3-yl）-2-methylpropanol derivatives were designed and synthesized based on 5-HT1A/SSRI drugs design strategies.The synthesized compounds were evaluated for their dual 5-HT1A/5-HTT activities.
