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

被引：7
作者：
Georgey, Hanan [1 ]
机构：
[1] Cairo Univ, Dept Pharmaceut Chem, Fac Pharm, Giza, Egypt
来源：
MOLECULES | 2014年 / 19卷 / 03期
关键词：
imidazolinone; imidazo[1,5-a]quinazoline; antitumor activity; Lipinski's parameters; 2D-QSAR; VITRO ANTITUMOR EVALUATION; BIOLOGICAL EVALUATION; KINASE INHIBITORS; ANALOGS; DESIGN; QUINAZOLINE;
D O I：
10.3390/molecules19033777
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
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.
引用
收藏
页码：3777 / 3792
页数：16
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