7-芳酰基氨基吲哚啉-1-磺酰胺类作为一类新型强效抗微管蛋白药物。

7-Aroyl-aminoindoline-1-sulfonamides as a novel class of potent antitubulin agents.

作者信息

Chang Jang-Yang, Hsieh Hsing-Pang, Chang Chi-Yen, Hsu Kuo-Shun, Chiang Yi-Fang, Chen Chi-Ming, Kuo Ching-Chuan, Liou Jing-Ping

机构信息

Institute of Cancer Research, National Health Research Institutes, Taipei, Taiwan, Republic of China.

出版信息

J Med Chem. 2006 Nov 16;49(23):6656-9. doi: 10.1021/jm061076u.

DOI:10.1021/jm061076u

PMID:17154496

Abstract

A novel series of 7-aroyl-aminoindoline-1-benzenesulfonamides showed excellent activity as inhibitors of tubulin polymerization through binding with the colchicine binding site of microtubules. Compound 15 and 16 display IC50 values of 1.1 and 1.2 microM, respectively. Compound 15 inhibited the human cancer cell growth of KB, MKN45, H460, HT29, and TSGH, as well as one human-resistant cancer line of KB-vin 10, with an IC50 of 9.6, 8.8, 9.4, 8.6, 10.8, and 8.9 nM, respectively.

摘要

一系列新型的7-芳酰基氨基吲哚啉-1-苯磺酰胺通过与微管的秋水仙碱结合位点结合，表现出作为微管蛋白聚合抑制剂的优异活性。化合物15和16的IC50值分别为1.1和1.2微摩尔。化合物15抑制KB、MKN45、H460、HT29和TSGH的人类癌细胞生长，以及KB-vin 10这一人类耐药癌细胞系，IC50分别为9.6、8.8、9.4、8.6、10.8和8.9纳摩尔。