2. Academic Validation
  3. 4- and 5-aroylindoles as novel classes of potent antitubulin agents

4- and 5-aroylindoles as novel classes of potent antitubulin agents

  • J Med Chem. 2007 Sep 6;50(18):4548-52. doi: 10.1021/jm070557q.
Jing-Ping Liou 1,  Chang-Ying Wu,  Hsing-Pang Hsieh,  Chi-Yen Chang,  Chi-Ming Chen,  Ching-Chuan Kuo,  Jang-Yang Chang
Affiliations

Affiliation

  • 1 College of Pharmacy, Taipei Medical University, Taipei 110, Taiwan, Republic of China.
PMID: 17685504 DOI: 10.1021/jm070557q
Abstract

A novel series of 4- and 5-aroylindole derivatives was prepared and evaluated for antitumor activity. Several compounds showed excellent antiproliferative activity as inhibitors of tubulin polymerization. Compounds 13, 14, 15, and 18, with IC50 values of 1.9, 1.1, 1.2, and 1.8 microM, respectively, exhibited more potent inhibition of tubulin polymerization than colchicine. They also displayed antiproliferative activity, with IC50 values ranging from 10 to 43 nM in a variety of human cell lines from different organs.

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