2. Academic Validation
  3. Discovery of 4-amino and 4-hydroxy-1-aroylindoles as potent tubulin polymerization inhibitors

Discovery of 4-amino and 4-hydroxy-1-aroylindoles as potent tubulin polymerization inhibitors

  • J Med Chem. 2008 Jul 24;51(14):4351-5. doi: 10.1021/jm800150d.
Jing-Ping Liou 1,  Zi-Yi Wu,  Ching-Chuan Kuo,  Chi-Yen Chang,  Pei-Yi Lu,  Chi-Ming Chen,  Hsing-Pang Hsieh,  Jang-Yang Chang
Affiliations

Affiliation

  • 1 College of Pharmacy, Taipei Medical University, Taipei 110, Taiwan, Republic of China.
PMID: 18588280 DOI: 10.1021/jm800150d
Abstract

1-Aroylindoline, 1-aroyl-1,2,3,4-tetrahydroquinoline, and 1-aroylindole derivatives were synthesized and evaluated for Anticancer activity. The 4-amino and 4-hydroxy-1-aroylindoles 26 and 27 with IC 50 of 0.9 and 0.6 microM, respectively, exhibited antitubulin activity superior or comparable to that of colchicine and combretastatin A-4. They also showed antiproliferative activity with IC 50 of 0.3-5.4 nM in a set of human Cancer cell lines.

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