The present invention refers to 4-amino-substituted pyrazolo[3,4-d]pyrimidine and pyrrolo[2,3-d]pyrimidine derivs. of formula I able to target the Src family kinases (SFKs) such as Src, Fyn and Hck tyrosine kinases as well as Abl tyrosine kinase and uses and method of prepn. thereof, wherein Z = CH or N; R2 = alkyl; Y = NH, O or S; X = CH or N; W = NH, NCH3 or S; n = 0-4; m = 0-1; R3 = H or aralkyl; R4 = substituted Ph. In particular, the compds. of the invention are for use in the treatment and/or prevention of cancer, such as neuroblastoma (NB) or glioblastoma multiform (GBM) or for use in the treatment and/or prevention of neurodegenerative diseases such as taupathies. Thus, e.g., II was prepd. and showed EC50 value of 0.20 μM against c-Src and 0.15 μM against Abl in enzymic activity assay.
Preparation of 4-amino-substituted pyrazolo[3,4-d]pyrimidine and pyrrolo[2,3-d]pyrimidine derivative as the Src family kinases
SCHENONE, SILVIA;
2016-01-01
Abstract
The present invention refers to 4-amino-substituted pyrazolo[3,4-d]pyrimidine and pyrrolo[2,3-d]pyrimidine derivs. of formula I able to target the Src family kinases (SFKs) such as Src, Fyn and Hck tyrosine kinases as well as Abl tyrosine kinase and uses and method of prepn. thereof, wherein Z = CH or N; R2 = alkyl; Y = NH, O or S; X = CH or N; W = NH, NCH3 or S; n = 0-4; m = 0-1; R3 = H or aralkyl; R4 = substituted Ph. In particular, the compds. of the invention are for use in the treatment and/or prevention of cancer, such as neuroblastoma (NB) or glioblastoma multiform (GBM) or for use in the treatment and/or prevention of neurodegenerative diseases such as taupathies. Thus, e.g., II was prepd. and showed EC50 value of 0.20 μM against c-Src and 0.15 μM against Abl in enzymic activity assay.
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