C6‐Unsubstituted Pyrazolo[3,4‐d]pyrimidines Are Dual Src/Abl Inhibitors Effective against Imatinib Mesylate Resistant Chronic Myeloid Leukemia Cell Lines

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...

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Veröffentlicht in:	ChemMedChem 2009-01, Vol.4 (1), p.118-126
Hauptverfasser:	Santucci, Maria Alessandra, Corradi, Valentina, Mancini, Manuela, Manetti, Fabrizio, Radi, Marco, Schenone, Silvia, Botta, Maurizio
Format:	Artikel
Sprache:	eng
Schlagworte:	Amino Acid Substitution Animals Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology Antineoplastic Agents - toxicity Benzamides Cell Line, Tumor chronic myeloid leukemia Computer Simulation Drug Resistance, Neoplasm enzymes Imatinib Mesylate inhibitors Leukemia, Myelogenous, Chronic, BCR-ABL Positive - drug therapy Mice Models, Molecular molecular modeling Mutation Phosphorylation Piperazines - pharmacology Protein Kinase Inhibitors - chemistry Protein Kinase Inhibitors - pharmacology Protein Kinase Inhibitors - toxicity Proto-Oncogene Proteins c-abl - antagonists & inhibitors Proto-Oncogene Proteins c-abl - chemistry pyrazolo[3,4‐d]pyrimidines Pyrimidines - chemistry Pyrimidines - pharmacology Pyrimidines - toxicity src-Family Kinases - antagonists & inhibitors src-Family Kinases - chemistry
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