Synthesis and biological evaluation of 2-aryl-4-aminoquinazolines as antitumor agents

Le Nguyen Thanh, Tran Huu Giap, Nguyen Anh Dung, Vu Thi Mung, Van Thi My Hue, Nguyen Thi Minh Hang, Chau Van Minh, Won-Jea Cho


Quinazoline is an important pharmacophore, showing many biological activities. Some novel 2-aryl-4-aminoquinazolines were designed from 3-arylisoquinoline-1-amines using bioisostere approach. The 4-aminoquinazoline derivatives were prepared from corresponding quinazolinones in 3 steps. The cytotoxicity of these compounds was evaluated against 4 cancer cell lines including human epidermic carcinoma (KB), hepatocellular carcinoma (Hep-G2),  human lung carcinoma (LU-1) and human breast carcinoma (MCF-7). Quinazolineamine compound 4a showed good antitumor activity on KB cell line.


Anticancer, 3-arylisoquinolinamine, 2-aryl-4-aminoquinazolines.

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