Synthesis and Biological Evaluation of 2-Substituted Quinazolin-4(3<i>H</i>)-Ones with Antiproliferative Activities

Abstract

Sixteen new 2-substituted quinazolines were synthesized using a straightforward methodology starting from 2-methoxybezoic acid or 3-methoxy-2-naphthoic acid. The anti-proliferative activity of the target compounds was evaluated against nine cancer cell lines. Additionally, all the compounds were screened for their potency and selectivity against a panel of 109 kinases and four bromodomains, using Differential Scanning Fluorimetry (DSF). Compound 17 bearing a 2-methoxyphenyl substitution along with a basic side chain displayed a remarkable profile against the majority of the tested cell lines.

Keywords

• quinazolines
• synthesis
• anti-proliferative activity
• kinase inhibition