Series of 2,4-disubstituted quinazoline and 2-substituted or 2,3-disubstituted quinazolin-4(3H)-one derivatives as antitumor agents were designed and synthesized. The structures of the newly synthesized compounds were elucidated by IR, 1H NMR, 13C NMR, mass spectroscopy and elemental analyses. The antitumor activity of the target compounds were evaluated using the National Cancer Institute disease oriented antitumor screening protocol. It was found that all the tested compounds showed activity against two cell lines (CNS and renal) and compound 21 was the most active derivative in this study with GI% 59.44 against HOP-92.
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