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ID: ALA1156102

Journal: Bioorg Med Chem Lett

Title: Identification of iminooxothiazolidines as secreted frizzled related protein-1 inhibitors.

Authors: Shi M, Stauffer B, Bhat R, Billiard J, Ponce-de-Leon H, Seestaller-Wehr L, Fukayama S, Mangine A, Moran R, Krishnamurthy G, Bodine P, Gopalsamy A.

Abstract: Secreted frizzled related protein-1 (sFRP-1) inhibitors have the potential to be used for the treatment of osteoporosis or other bone related disorders, since the level of sFRP-1 affects osteoblast apoptosis and proliferation. From high throughput screening, we have identified a class of iminooxothiazolidines as sFRP-1 inhibitors. Structure-activity relationships were established for various regions of the scaffold along with the biochemical characterization of this class to probe selectivity, binding and ex vivo activity.

CiteXplore: 19819694

DOI: 10.1016/j.bmcl.2009.09.085