Synthesis, biological evaluation and docking studies of 4-amino-tetrahydroquinazolino[3,2-e]purine derivatives

被引：6

作者：

Verones, Valerie ^{[1
]}

Flouquet, Nathalie ^{[1
]}

Farce, Amaury ^{[1
]}

Carato, Pascal ^{[1
]}

Leonce, Stephane ^{[2
]}

Pfeiffer, Bruno ^{[2
]}

Berthelot, Pascal ^{[1
]}

Lebegue, Nicolas ^{[1
]}

机构：

[1] Fac Sci Pharmaceut & Biol Lille, Chim Therapeut Lab, F-59000 Lille, France

[2] Div Rech Cancerol, Inst Rech SERVIER, F-78290 Croissy Sur Seine, France

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2010年 / 45卷 / 12期

关键词：

Aminopurine; Src; Cytotoxic; Docking; TYROSINE KINASE INHIBITORS; ANTIRHINOVIRUS ACTIVITY; INTERFERON INDUCERS; C-SRC; POTENT; PURINES; VALIDATION; DESIGN; 9-BENZYLADENINE; PREDICTION;

D O I：

10.1016/j.ejmech.2010.09.022

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthesis of new 4-amino-tetrahydroquinazolino[3,2-e]purine derivatives along with their activity in cell-free enzymatic assays on Src is reported. Some compounds emerged as moderately active inhibitors of the enzyme and showed antiproliferative effects on the murine leukemia L1210 cell line. Docking studies have been also performed to analyze the binding mode of compounds under study and to identify the structural determinants of their interaction. Therefore, this study provides a new promising scaffold with moderate enzymatic inhibitory activities for further development of new anticancer drugs targeting Src tyrosine kinase. (C) 2010 Elsevier Masson SAS. All rights reserved.

引用

页码：5678 / 5684

页数：7

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