新型N-取代苯基-9-烷基-3-咔唑磺酰脲类化合物的合成及其抗肿瘤活性

Synthesis and Antitumor Activities of Novel N-substituted Phenyl-9-alkyl-3-carbazole Sulfonylureas

以9-烷基咔唑为原料,经磺化、氯化和氨化反应制得9-烷基咔唑-3-磺酰胺(4a和4o);取代苯胺与三光气反应制得取代苯基异氰酸酯(6a^6n,6s,6Ⅳ);4分别与6经缩合反应合成了30个新型的N-取代苯基-9-烷基-3-咔唑磺酰脲类化合物(7a^7Ⅳ),其结构经1H NMR,IR和ESI-MS表征。对7进行了Cdc25B抑制活性筛选。结果表明,在用药浓度为20μg·m L-1时,其中12个化合物对Cdc25B具有良好的抑制活性,抑制率大于90%。

9-Alkyl carbazole-3-sulfonamides（ 4a and 4o） were synthesized by sulfonation,chlorination and ammonifination from 9-alkyl carbazole. A series of substituted phenylisocyanates（ 6a ～ 6n,6s,6Ⅳ） were obtained by reaction of substituted anilines with triphosgene. Finally,thirty novel N-substituted phenyl-9-alkyl-3-carbazole sulfonylureas（ 7a ～ 7 Ⅳ） were synthesized by condensation of 4with 6,respectively. The structures were characterized by1 H NMR,IR and ESI-MS. 7 were screened for Cdc25 B inhibitory activities. The results showed that twelve compounds of them exhibited better inhibitory activities to Cdc25 B with the inhibition rate of more than 90% at 20 μg·mL^-1.