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

  title={Synthesis, biological evaluation and docking studies of 4-amino substituted 1H-pyrazolo[3,4-d]pyrimidines.},
  author={Silvia Schenone and Chiara Brullo and O. A. Bruno and Francesco Bondavalli and Luisa Mosti and Giovanni Maga and Emmanuele Crespan and Fabio Carraro and Fabrizio Manetti and Cristina Tintori and Maurizio Botta},
  journal={European journal of medicinal chemistry},
  volume={43 12},
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… CONTINUE READING

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