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Eur J Med Chem. 2008 Dec;43(12):2665-76. doi: 10.1016/j.ejmech.2008.01.034. Epub 2008 Feb 6.

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

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  • 1Dipartimento di Scienze Farmaceutiche, Universit√† degli Studi di Genova, Viale Benedetto XV 3, I-16132 Genova, Italy.


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.

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