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. 2009 Jan 8;52(1):105-16.
doi: 10.1021/jm801144h.

Modulation of Wnt Signaling Through Inhibition of Secreted Frizzled-Related Protein I (sFRP-1) With N-substituted Piperidinyl Diphenylsulfonyl Sulfonamides

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Modulation of Wnt Signaling Through Inhibition of Secreted Frizzled-Related Protein I (sFRP-1) With N-substituted Piperidinyl Diphenylsulfonyl Sulfonamides

William J Moore et al. J Med Chem. .

Abstract

The diphenylsulfonyl sulfonamide scaffold represented by 1 (WAY-316606) are small molecule inhibitors of the secreted protein sFRP-1, an endogenous antagonist of the secreted glycoprotein Wnt. Modulators of the Wnt pathway have been proposed as anabolic agents for the treatment of osteoporosis or other bone-related disorders. Details of the structure-activity relationships and biological activity from the first structural class of this scaffold will be discussed.

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