Design, Synthesis and Anticancer Activity of Novel 6-（Aminophenyl）-2,4-bismorpholino-1,3,5-triazine Derivatives Bearing Arylmethylene Hydrazine Moiety  

作　　者：HUANG Qiang FU Qiangqiang LIU Yajing BAI Jinying WANG Qianying LIAO Huimin GONG Ping 

机构地区：[1]Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education,Shenyang Pharmaceutical University, Shenyang 110016, P.R.China

出　　处：《Chemical Research in Chinese Universities》2014年第2期257-265,共9页高等学校化学研究（英文版）

摘　　要：In an attempt to develop potent and selective anticancer agents,we designed and synthesized a series of novel bis（morpholino-1,3,5-triazine） derivatives beating aylmethylene hydrazine moiety and evaluated their cytotoxicity,in vitro,against H460（non-small-cell lung cancer）,HT-29（human colorectal cancer） and MDA-MB-231（human breast cancer） cell lines.The pharmacological results indicate that all the compounds exhibit enhanced cytotoxicity than BMCL-200908069-1,and six target compounds（7e,7h,7j,9a,9b,9c） were superior to PAC-1 against all the tested cancer cell lines.The most active compound 7j,with IC50（inhibitory concentration 50％）values of 0.75,0.34 and 0.60 μ mol/L against HT-29,H460 and MDA-MB-231 cancer cell lines,was 39-,28-,and 60-fold more potent than BMCL-200908069-1 （29.24,9.52 and 36.21 μmol/L）,respectively.In an attempt to develop potent and selective anticancer agents,we designed and synthesized a series of novel bis（morpholino-1,3,5-triazine） derivatives beating aylmethylene hydrazine moiety and evaluated their cytotoxicity,in vitro,against H460（non-small-cell lung cancer）,HT-29（human colorectal cancer） and MDA-MB-231（human breast cancer） cell lines.The pharmacological results indicate that all the compounds exhibit enhanced cytotoxicity than BMCL-200908069-1,and six target compounds（7e,7h,7j,9a,9b,9c） were superior to PAC-1 against all the tested cancer cell lines.The most active compound 7j,with IC50（inhibitory concentration 50％）values of 0.75,0.34 and 0.60 μ mol/L against HT-29,H460 and MDA-MB-231 cancer cell lines,was 39-,28-,and 60-fold more potent than BMCL-200908069-1 （29.24,9.52 and 36.21 μmol/L）,respectively.

关 键 词：Bis（morpholino-1 3 5-triazine） DESIGN Anticancer activity 

分 类 号：TQ314.248[化学工程—高聚物工业] TQ226.52