Title of article
Bone-Targeted pyrido[2,3-d]pyrimidin-7-ones: potent inhibitors of Src tyrosine kinase as novel antiresorptive agents
Author/Authors
Chi B. Vu، نويسنده , , George P. Luke، نويسنده , , Noriyuki Kawahata، نويسنده , , William C. Shakespeare، نويسنده , , Yihan Wang، نويسنده , , Raji Sundaramoorthi، نويسنده , , Chester A. Metcalf III، نويسنده , , Terence P. Keenan، نويسنده , , Selvi Pradeepan، نويسنده , , Evelyn Corpuz، نويسنده , , Taylor Merry، نويسنده , , Regine S. Bohacek، نويسنده , , David C. Dalgarno، نويسنده , , Surinder S. Narula، نويسنده , , Marie-Rose van Schravendijk، نويسنده , , Mary K. Ram، نويسنده , , Susan Adams، نويسنده , , Shuenn Liou، نويسنده , , Jeffrey A. Keats، نويسنده , , Shelia M. Violette، نويسنده , , et al.، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2003
Pages
4
From page
3071
To page
3074
Abstract
The design of bone-targeted pyrido[2,3-d]pyrimidin-7-ones as Src tyrosine kinase inhibitors is described. Leveraging SAR from known compounds and using structure-based methods, we were able to rapidly incorporate bone binding components, which maintained, and even increased potency against the target enzyme. Compound 4 displayed a high affinity for hydroxyapatite, a major constituent of bone, and demonstrated antiresoprtive activity in our cell-based assay.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2003
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
793511
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