The enzymatic synthesis of CCK-8 tripeptide derivative Phac-Met-Asp(OMe)-Phe-NH2 is reported. Starting with Phac-Met-OCam, we have successfully synthesized the target tripeptide with three free or immobilized enzymes...The enzymatic synthesis of CCK-8 tripeptide derivative Phac-Met-Asp(OMe)-Phe-NH2 is reported. Starting with Phac-Met-OCam, we have successfully synthesized the target tripeptide with three free or immobilized enzymes, ?chymotrypsin, papain and thermolysin in reasonable yields. The key steps in this synthesis were the coupling of Phac-Met-OCam and H-Asp(OMe)2 to form Met-Asp peptide bond catalyzed by ?chymotrypsin and the selective hydrolysis of -ester of Phac-Met-Asp(OMe)2 catalyzed by papain.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
文摘The enzymatic synthesis of CCK-8 tripeptide derivative Phac-Met-Asp(OMe)-Phe-NH2 is reported. Starting with Phac-Met-OCam, we have successfully synthesized the target tripeptide with three free or immobilized enzymes, ?chymotrypsin, papain and thermolysin in reasonable yields. The key steps in this synthesis were the coupling of Phac-Met-OCam and H-Asp(OMe)2 to form Met-Asp peptide bond catalyzed by ?chymotrypsin and the selective hydrolysis of -ester of Phac-Met-Asp(OMe)2 catalyzed by papain.
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.
