2. Academic Validation
  3. 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

  • J Med Chem. 2006 Nov 16;49(23):6656-9. doi: 10.1021/jm061076u.
Jang-Yang Chang 1,  Hsing-Pang Hsieh,  Chi-Yen Chang,  Kuo-Shun Hsu,  Yi-Fang Chiang,  Chi-Ming Chen,  Ching-Chuan Kuo,  Jing-Ping Liou
Affiliations

Affiliation

  • 1 Institute of Cancer Research, National Health Research Institutes, Taipei, Taiwan, Republic of China.
PMID: 17154496 DOI: 10.1021/jm061076u
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.

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