7-aroyl-aminoindoline-1-sulfonamides as a novel class of potent antitubulin agents
7-aroyl-aminoindoline-1-sulfonamides as a novel class of potent antitubulin agents
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DOI：
10.1021/jm061076u
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发表时间：
2006-11-16
影响因子：
7.3
通讯作者：
Liou, Jing-Ping
中科院分区：
文献类型：
--
作者：
Chang, Jang-Yang;Hsieh, Hsing-Pang;Liou, Jing-Ping
一系列新的7-芳酰基-氨基吲哚啉-1-苯磺酰胺类化合物通过与微管的秋水仙碱结合位点结合，显示出作为微管蛋白聚合抑制剂的优异活性。化合物15和16显示的IC 50值分别为1.1和1.2 μ M。化合物15抑制KB、MKN 45、H460、HT 29和TSGH的人癌细胞生长，以及KB-vin 10的一种人耐药癌细胞系，IC 50分别为9.6、8.8、9.4、8.6、10.8和8.9 nM。
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 mu M, 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.