N'-取代苯基-4-甲氧基苯磺酰脲类化合物的合成及其对Cdc25B抑制活性研究  

Synthesis and antitumor activities of N'-substituted phenyl-4-methoxybenzenesulfonylureas

作　　者：于姝燕[1] 马丽娟[2] 巴俊杰[1] 王敏[1] 

机构地区：[1]内蒙古医科大学药学院,内蒙古呼和浩特010110 [2]包钢集团第三职工医院,内蒙古包头014010

出　　处：《化学研究与应用》2016年第12期1712-1717,共6页Chemical Research and Application

基　　金：内蒙古自治区自然科学基金项目(2013MS1210)资助;内蒙古医科大学高等教育教学改革项目(NYJXGG2016050)资助

摘　　要：以苯甲醚为原料,经氯磺化、氨化反应制得4-甲氧基苯磺酰胺3;取代苯胺与三光气反应制得取代苯基异氰酸酯5a^5q;5分别与3经缩合反应合成了17个新型的N'-取代苯基-4-甲氧基苯磺酰脲类化合物6a^6q,其结构经MS、IR和1H NMR表征确证。通过抗肿瘤活性初步测试,其中有5个化合物对Cdc25B具有一定的抑制作用。4-Methoxybenzenesulfonamide 3 were synthesized by chlorosulfonation,ammonifination from anisole.A series of substituted phenylisocyanates 5a - 5q were obtained by reaction of substituted anilines with triphosgene（ BTC）. Finally,seventeen novel N＇-substituted phenyl-4-methoxybenzenesulfonylureas 6a - 6q were synthesized by condensation of 5 with 3,respectively.The structures of target compounds were characterized by MS,IR,and1 H NMR.Preliminary antitumor activity test showed that five compounds of them had relatively inhibitory activities to Cdc25 B.

关 键 词：N'-取代苯基-4-甲氧基苯磺酰脲 合成 CDC25B 

分 类 号：O623.84[理学—有机化学]