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Bone-targeted pyrido[2,3-d]pyrimidin-7-ones: potent inhibitors of Src tyrosine kinase as novel antiresorptive agents. 2003
Chi B Vu, and
George P Luke, and
Noriyuki Kawahata, and
William C Shakespeare, and
Yihan Wang, and
Raji Sundaramoorthi, and
Chester A Metcalf, and
Terence P Keenan, and
Selvi Pradeepan, and
Evelyn Corpuz, and
Taylor Merry, and
Regine S Bohacek, and
David C Dalgarno, and
Surinder S Narula, and
Marie Rose van Schravendijk, and
Mary K Ram, and
Susan Adams, and
Shuenn Liou, and
Jeffrey A Keats, and
Shelia M Violette, and
Wei Guan, and
Manfred Weigele, and
Tomi K Sawyer
ARIAD Pharmaceuticals, Inc., 26 Landsdowne Street, Cambridge, MA 02139-4234, USA.
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.
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Heliyon,
