Design, Synthesis, Characterization, Molecular Docking Studies and Biological Activity of Novel Quinazolinone Derivatives as Potential Egfr Inhibitors

Abstract

A series of novel quinazolinone derivatives [(E)-7-chloro-2-(4-((4-substituted benzylidene) amino) phenyl) quinazolin-4(3H)-one] were synthesised, characterized and biological screened for their in vitro antibacterial, anthelmintic and anticancer activity. All compounds, were synthesized through two steps process and structurally conformed by FTIR, 1 HNMR and Mass spectroscopy. Their anticancer activity was assessed using MTT method against MCF-7 and SKOV3 cell lines, the anthelmintic activity was carried out by using Indian Earth warms and the antibacterial activity was carried out by Cup-plate diffusion method. In addition, molecular docking studies was assessed using Autodock Vina. The compound II-3c (IC50 value of 23.24µg against MCF-7 and 21.05µg against SKVO3) exhibited good anticancer activity compared with Doxorubicin as standard. In anthelmintic and antibacterial screening, the compounds, II-3c, II-3h and II-3j have shown excellent anthelmintic activity and compounds II-3b, II-3d, II-3f, II-3h and II-3j showed significant antibacterial activity.