2. Academic Validation
  3. 5-Amino-2-aroylquinolines as highly potent tubulin polymerization inhibitors

5-Amino-2-aroylquinolines as highly potent tubulin polymerization inhibitors

  • J Med Chem. 2010 Mar 11;53(5):2309-13. doi: 10.1021/jm900685y.
Chih-Ying Nien 1,  Yun-Ching Chen,  Ching-Chuan Kuo,  Hsing-Pang Hsieh,  Chi-Yen Chang,  Jian-Sung Wu,  Su-Ying Wu,  Jing-Ping Liou,  Jang-Yang Chang
Affiliations

Affiliation

  • 1 College of Pharmacy, Taipei Medical University, Taipei 110, Taiwan, Republic of China.
PMID: 20148562 DOI: 10.1021/jm900685y
Abstract

A series of aroylquinoline derivatives were synthesized and evaluated for Anticancer activity. 5-Amino-6-methoxy-2-aroylquinoline 15 showed more potent antiproliferative activity (IC(50) values ranging from 0.2 to 0.4 nM) as compared to 1a (combretastatin A-4) (IC(50) = 1.9-835 nM) against various human Cancer cell lines and a MDR-resistant Cancer cell line. Compound 15 (IC(50) = 1.6 microM) exhibited more potent inhibition of tubulin polymerization than 1a (IC(50) = 2.1 microM) and showed strong binding property to the colchicine binding site of microtubules.

Figures