Please use this identifier to cite or link to this item: http://hdl.handle.net/20.500.12779/5512
Title: Synthesis, biological evaluation and docking studies of 4-amino substituted 1H-pyrazolo[3,4-d]pyrimidines.
Authors: Schenone, S
Brullo, C
Bruno, O
Bondavalli, F
Mosti, L
Maga, G
Crespan, E
Carraro, Fabio
Manetti, Fabrizio 
Tintori, C
Botta, Maurizio 
Keywords: Abl; Chronic myeloid leukemia; Docking; Pyrazolo-pyrimidines; Src
Issue Date: 2008
Project: None 
Journal: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Abstract: 
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.
Description: 
37870
URI: http://hdl.handle.net/20.500.12779/5512
ISSN: 0223-5234
DOI: 10.1016/j.ejmech.2008.01.034
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