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.pdfVIP

学兔兔 2015年第23卷 合成化学 Vo1．23，2015 第5期，369—375 Chinese Journal of Synthetic Chemistry No．5，369—375 · 研究论文· 新型Ⅳ-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 钱 宇，田 静，常霄巍，巴俊杰 (内蒙古医科大学药学院，内蒙古呼和浩特 010110) 摘要：以9．烷基咔唑为原料，经磺化、氯化和氨化反应制得9-烷基咔唑一3-磺酰胺(4a和40)；取代苯胺与三光气 反应制得取代苯基异氰酸酯(ta一6n，6s，6IV)；4分别与6经缩合反应合成了30个新型的Ⅳ_取代苯基-9-烷基一 3一咔唑磺酰脲类化合物(7a一7rv)，其结构经。H 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20 ·mL 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％。 关 键 词：9．烷基咔唑；Ⅳ_取代苯基-9-烷基-3．咔唑磺酰脲；合成；抗肿瘤活性 中图分类号：0625；O621．3 文献标识码：A DOI：10．15952／j．cnki．cj sc．1005—1511．2015．05．0369 Synthesis and Antitumor Activities of Novel N—substituted Phenyl一9一alky1-3-carbazole Sulfonylureas QIAN Yu，TIAN Jing， CHANG Xiao-wei， BA Jun,jie (School of Pharmacy，Inner Mongolia Medical University，Hohhot 0101 10，China) Abstract：9-Alkyl carbazole-3一sulfonamides(4a and 40)were synthesized by sulfonation，chlorination and ammonifination from 9一alkyl carbazole．A series of substituted phenylisocyanates(6a一6n，6s， 6 IV)were obtained by reaction of substituted anilines with triphosgene．Finally，thirty novel N-sub— stituted phenyl-9一alkyl-3一carbazole sulfonylureas(7a一7 IV)were synthesized by condensation of 4 with 6，respectively．The structures were characterized by H NMR，IR and ESI—MS．7 were screened for Cde25B inhibitory activities．The results showed that twelve compounds of them exhibited better inhibitory activities to Cdc25B with the inhibition rate of more than 90％ at 20 ·mL～． Keywords：9-alkyl carbazole；N-substituted phenyl-9一alkyl-3一carbazole sulfonylurea；synthesis；an—