Design, synthesis and cytotoxic evaluation of novel imidazolone fused quinazolinone derivatives

Abstract

A congeneric series of novel imidazolone fused quinazolinone derivatives were synthesized and characterized by IR, NMR, mass spectra and elemental analyses. All the compounds were evaluated for their in vitro cytotoxic activity against cervical cancer (HeLa), breast cancer (MCF-7), leukemia cells (HL-60) and hepatocellular carcinoma (HepG2) cell lines. The derivative 4e which bears a methoxy group at para position in phenyl ring of imidazolone displayed three fold potent activity against MCF-7 than that of the standard drug Cisplatin. The IC50 value of 4e against HepG2 is twofold lesser than Cisplatin whereas the IC50 value against HeLa and HL-60 was equivalent to Cisplatin. The result concludes that these derivatives can be further utilized as a promising anticancer agent.

Keywords

• Quinazolinones
• Anticancer
• Anti-HIV
• Breast cancer
• Hepatocellular carcinoma