- Identification of iminooxothiazolidines as secreted frizzled related protein-1 inhibitors.
Identification of iminooxothiazolidines as secreted frizzled related protein-1 inhibitors.
Bioorganic & medicinal chemistry letters (2009-10-13)
Mengxiao Shi, Barbara Stauffer, Ramesh Bhat, Julia Billiard, Helga Ponce-de-Leon, Laura Seestaller-Wehr, Shoichi Fukayama, Annamarie Mangine, Robert Moran, Girija Krishnamurthy, Peter Bodine, Ariamala Gopalsamy
PMID19819694
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.
MATERIALS