Synthesis, anti-HIV and cytotoxic activities of 2-phenyl, 3-substituted quinazolin-4(3H)-ones


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3

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1

Abstract :

A series of novel 2,3-disubstitutedquinazolin-4(3H)-ones have been synthesized by condensation of 2-substituted benzo[1,3]oxazine-4-ones and primary amines. Their chemical structures were assigned by means of spectral analysis (FT-IR, 1H-NMR). Synthesized compounds were screened for in vitro antiviral activity against HIV -1 and -2 in MT-4 cells. Cytotoxicity of test compounds against mock-infected MT-4 cells (C type adult T leukemia cells) was also assessed by the MTT method. Anticancer activity also tested against Human liver cancer cells by MTT assay. Compound Q-2ABT (CC50:10.07±0.60) was found to be more toxic in this series in MT-4 cells. All the tested compounds exhibited significant cytotoxicity against liver cancer cells (CTC50: 150-206 µg/ml). Among all the nine compounds tested, Q-2ABT (158.81±3.46 µg/ml) showed better cytotoxicity against HepG2 (human liver cancer cells), where as standard Cis-platin was found to be 11.09±0.59 µg/ml (15 fold higher). Compound Q-2ABT merits further investigation to screen for their anticancer property.
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