الفهرس 
Design, Molecular Modeling, Synthesis and Anticancer Activity Evaluation of New Quinazoline Derivatives Incorporating Other Heterocycles
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Abstract
A novel series of 2-methyl-3-phenylquinazolin-4-one derivatives were synthesized via different synthetic approaches using 3-(4-acetylphenyl)-2-methylquinazolin-4(3H)-one II and 6-(un)substituted 3-(4-aminophenyl)-6-(un)substituted-2-methylquinazolin-4(3H)-one XVIa,b as starting materials. selected representative compounds for each series were biologically evaluated for their cytotoxic activity against three cancer cell lines (breast cancer MCF-7, liver cancer HepG-2 and prostate cancer PC-3). The most potent derivatives were subjected to cell division analysis, cell cycle progression analysis and apoptotic assay. All the tested compounds displayed cell division inhibition in dose-dependent manner, moreover, they caused cell cycle arrest at pre-G1 and G2/M phases and induced apoptosis. Furthermore, these compounds showed potent EGFR inhibitory activity at nanomolar concentrations. Finally, Molecular modeling simulations were performed to the most promising compounds revealing that all the target compounds possess a common binding pattern similar to that of Erlotinib.