Synthesis and antiproliferative evaluation of certain indolo[3,2-c]quinoline derivatives
作者:Chih-Ming Lu、Yeh-Long Chen、Hui-Ling Chen、Chyi-An Chen、Pei-Jung Lu、Chia-Ning Yang、Cherng-Chyi Tzeng
DOI:10.1016/j.bmc.2010.01.033
日期:2010.3
The present report describes the synthesis and antiproliferative evaluation of certain indolo[3,2-c]quinoline derivatives. For the C6 anilino-substituted derivatives, (11H-indolo[3,2-c]quinolin-6-yl)phenylamine (6a) was inactive. Structural optimization of 6a by the introduction of a hydroxyl group at the anilino-moiety resulted in the enhancement of antiproliferative activity in which the activity
本报告描述了某些吲哚并[3,2- c ]喹啉衍生物的合成和抗增殖评价。对于C 6苯胺基取代的衍生物,(11 H-吲哚并[3,2 - c ]喹啉-6-基)苯胺(6a)是不活泼的。通过在苯胺基部分引入羟基来优化6a的结构导致抗增殖活性增强,其中活性按对-OH,7a > 间位-OH,8a > 邻位-OH,9a的顺序降低。对于C 6烷基氨基取代的衍生物11a,12a,13a,14a和15a对所有测试的癌细胞和底特律551皮肤正常成纤维细胞均表现出相当的抗增殖活性。HeLa,A549和SKHep这三种癌细胞非常敏感,IC 50小于2.17μM,而PC-3对这组吲哚[3,2- c ]喹啉具有相对抗性。对于-2-苯乙氨基衍生物,化合物20A是对HeLa细胞的具有IC的生长活性50 0.52μM的,但是对活塞551的与IC生长不太有效50为19.32μM。对于双吲哚并[3,2- Ç〕喹啉,Ñ,ñ -双-