Synthesis, biological evaluation and docking studies of 4-amino substituted 1H-pyrazolo[3,4-d]pyrimidines

被引：68

作者：

Schenone, Silvia ^{[1
]}

Brullo, Chiara ^{[1
]}

Bruno, Olga ^{[1
]}

Bondavalli, Francesco ^{[1
]}

Mosti, Luisa ^{[1
]}

Maga, Giovanni ^{[2
]}

Crespan, Ernmanuele ^{[2
]}

Carraro, Fabio ^{[3
]}

Manetti, Fabrizio ^{[4
]}

Tintori, Cristina ^{[4
]}

Botta, Maurizio ^{[4
]}

机构：

[1] Univ Genoa, Dipartimento Sci Farmaceut, I-16132 Genoa, Italy

[2] IGM CNR, Ist Genet Mol, I-27100 Pavia, Italy

[3] Univ Siena, Dipartimento Fisiol, I-53100 Siena, Italy

[4] Univ Siena, Dipartimento Farmaco Chim Tecnol, I-53100 Siena, Italy

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2008年 / 43卷 / 12期

关键词：

Abl; Src; Pyrazolo-pyrimidines; Chronic myeloid leukemia; Docking;

D O I：

10.1016/j.ejmech.2008.01.034

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthesis of new 4-amino substituted pyrazolo[3,4-d]pyrimidines along with their activity in cell-free enzymatic assays on Src and Abl tyrosine kinases is reported. Some compounds emerged as good dual inhibitors of the two enzymes, showed antiproliferative effects on two Bcr-Abl positive leukemia cell lines K-562 and KU-812, and induced apoptosis, as demonstrated by the PARP assay. Docking studies have been also performed to analyze the binding mode of compounds under study and to identify the structural determinants of their interaction with both Src and Abl. (C) 2008 Elsevier Masson SAS. All rights reserved.

引用

页码：2665 / 2676

页数：12

共 49 条

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