Synthesis, cytotoxic activity and 2D-QSAR study of some imidazoquinazoline derivatives

Abstract

A novel series of 4-substituted amino-7,8-dimethoxy-1-phenylimidazo[1,5- a]quinazolin-5(4H)-one derivatives was designed, synthesized and tested for their antitumor activity against a human mammary carcinoma cell line (MCF7). Compound 5a was found to be the most active derivative. Physico-chemical parameters were also determined and revealed that most of the compounds obeyed the "rule of five" properties with good absorption percentages. 2D-QSAR studies revealed a well predictive and statistically significant and cross validated QSAR model that helps to explore some expectedly potent compounds. © 2014 by the authors; licensee MDPI, Basel, Switzerland.