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Molecules 2014, 19(3), 3777-3792; doi:10.3390/molecules19033777

Synthesis, Cytotoxic Activity and 2D-QSAR Study of Some Imidazoquinazoline Derivatives

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Cairo University, Cairo P.O. Box 11562, Egypt
Received: 14 January 2014 / Revised: 17 March 2014 / Accepted: 19 March 2014 / Published: 24 March 2014
(This article belongs to the Section Medicinal Chemistry)
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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.
Keywords: imidazolinone; imidazo[1,5-a]quinazoline; antitumor activity; Lipinski’s parameters; 2D-QSAR imidazolinone; imidazo[1,5-a]quinazoline; antitumor activity; Lipinski’s parameters; 2D-QSAR
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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Georgey, H. Synthesis, Cytotoxic Activity and 2D-QSAR Study of Some Imidazoquinazoline Derivatives. Molecules 2014, 19, 3777-3792.

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