AI Article Synopsis
- Novel inhibitors targeting Src tyrosine kinase based on a purine template have been developed.
- Drug design focused on enhancing bone-targeting capabilities by modifying specific positions (2 and 6) of known purine compounds.
- Compound 3d emerged as a strong Src inhibitor, demonstrating selectivity over various other protein kinases.
Article 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.
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| http://dx.doi.org/10.1016/s0960-894x(03)00648-6 | DOI Listing |
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