SYNTHESIS AND CYTOTOXIC ACTIVITY OF N-(BROMOPHENYL)-6-FLUOROQUINAZOLIN-4-AMINE DERIVATIVES AGAINST CANCER CELLS

Abstract

Quinazoline and its derivatives have demonstrated considerable anticancer potential. The incorporation of halogen atoms into aromatic scaffolds is recognized for enhancing pharmacokinetic properties, including potency, metabolic stability, and target selectivity. In the present work, a series of novel quinazoline-based compounds were synthesized through a concise three-step synthetic route, commencing from 5-fluoro-2-nitrobenzaldehyde. The synthesized compounds were assessed for their in vitro cytotoxicity against two human cancer cell lines: hepatocellular carcinoma (HepG2) and lung adenocarcinoma (A549). Notably, the ortho-brominated derivative (compound Va) exhibited markedly higher anticancer activity compared to its meta- and para-substituted counterparts.