N′-取代苯基-4-甲氧基苯磺酰脲类化合物的合成及其对Cdc25 B抑制活性研究

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1 H 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 substitu-ted 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,and 1 H NMR. Preliminary antitumor activity test showed that five compounds of them had relatively inhibitory activities to Cdc25B.