Identification of iminooxothiazolidines as secreted frizzled related protein-1 inhibitors

…, J Billiard, H Ponce-de-Leon, L Seestaller-Wehr…

Index: Shi, Mengxiao; Stauffer, Barbara; Bhat, Ramesh; Billiard, Julia; Ponce-de-Leon, Helga; Seestaller-Wehr, Laura; Fukayama, Shoichi; Mangine, Annamarie; Moran, Robert; Krishnamurthy, Girija; Bodine, Peter; Gopalsamy, Ariamala Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 22 p. 6337 - 6339

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Citation Number: 8

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 ...