Title of article :
Bone-Targeted 2,6,9-Trisubstituted purines: novel inhibitors of Src tyrosine kinase for the treatment of bone diseases
Author/Authors :
Yihan Wang، نويسنده , , Chester A. Metcalf III، نويسنده , , William C. Shakespeare، نويسنده , , Raji Sundaramoorthi، نويسنده , , Terence P. Keenan، نويسنده , , Regine S. Bohacek، نويسنده , , Marie-Rose van Schravendijk، نويسنده , , Shiela M. Violette، نويسنده , , Surinder S. Narula، نويسنده , , David C. Dalgarno، نويسنده , , Chad Haraldson، نويسنده , , Jeffrey Keats، نويسنده , , Shuenn Liou، نويسنده , , Ukti Mani، نويسنده , , Selvi Pradeepan، نويسنده , , Mary Ram، نويسنده , , Susan Adams، نويسنده , , Manfred Weigele، نويسنده , , Tomi K. Sawyer، نويسنده ,
Abstract :
Novel bone-targeted 2,6,9-trisubstituted purine template-based inhibitors of Src tyrosine kinase are described. Drug design studies of known purine compounds revealed that both positions-2 and -6 were suitable for incorporating bone-seeking moieties. A variety of bone-targeting groups with different affinity to hydroxyapatite were utilized in the study. Compound 3d was determined to be a potent Src inhibitor and was quite selective against a panel of other protein kinases.
