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Updated: Jun 16, 2026

Optimizing Tubulin Yield from Porcine Brain Tissue
Published on: October 11, 2024
5-Amino-2-aroylquinolines as highly potent tubulin polymerization inhibitors
Chih-Ying Nien1, Yun-Ching Chen, Ching-Chuan Kuo
1College of Pharmacy, Taipei Medical University, Taipei 110, Taiwan, Republic of China.
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.
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