Article
C6-unsubstituted pyrazolo[3,4-d]pyrimidines are dual Src/Abl inhibitors effective against imatinib mesylate resistant chronic myeloid leukemia cell lines.
ChemMedChem - 1 Jan 2009
Santucci Maria Alessandra, Corradi Valentina, Mancini Manuela, Manetti Fabrizio, Radi Marco, Schenone Silvia, Botta Maurizio
Abstract excerpt
Docking simulations were used to predict the most favorable interaction between the T315I mutated form of Abl (invariably associated with resistance to the tyrosine kinase inhibitor imatinib mesylate, IM) and C6-unsubstituted and substituted pyrazolo[3,4-d]pyrimidines previously found to be dual Src/Abl inhibitors. Two C6-unsubstituted (1 and 2) and eight C6-substituted compounds (3-10) were selected and assayed...
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