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Updated: May 21, 2026

Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
Design, synthesis and cytotoxicity of novel 2-arylvinyl-4-aminoquinoline derivatives
Nan Jiang1, Xin Zhai, Zhichao Chen
1Key Lab of New Drugs Design and Discovery of Liaoning Province, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang, P. R. China.
Abstract:
With an aim to develop promising anti-tumor agents, a novel series of 2-arylvinyl-4-aminoquinoline derivatives were designed, synthesized and evaluated for their cytotoxicity against H-460, HT-29, HepG2 and SGC-7901 cell lines in vitro. The pharmacological results indicated that most compounds were more potent than the positive controls, especially compounds 8, 14 and 16 with IC(50) values ranging from 0.05 to 0.85 µM against all tested cell lines respectively, which were 5.7- to 112-fold better than Iressa. The most active compound 14 (IC(50) values of 0.05, 0.25, 0.16, 0.68 µM), bearing 4-fluorostyryl at C-2 position and 3-(dimethylamino)-1-propylamino at C-4 position, showed great promise as a lead for the development of more effective quinoline analogues.
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