4.7 Article

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

Journal

JOURNAL OF MEDICINAL CHEMISTRY
Volume 49, Issue 23, Pages 6656-6659

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/jm061076u

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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.

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