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

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 which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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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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