Modulation of Wnt signaling through inhibition of secreted frizzled-related protein I (sFRP-1) with N-substituted piperidinyl diphenylsulfonyl sulfonamides

  • J Med Chem. 2009 Jan 8;52(1):105-16. doi: 10.1021/jm801144h.
William J Moore  1 ,  Jeffrey C Kern ,  Ramesh Bhat ,  Thomas J Commons ,  Shoichi Fukayama ,  Igor Goljer ,  Girija Krishnamurthy ,  Ronald L Magolda ,  Lisa Nogle ,  Keith Pitts ,  Barb Stauffer ,  Eugene J Trybulski ,  Gregory S Welmaker ,  Matthew Wilson ,  Peter V N Bodine
Affiliations
  • 1. Chemical and Screening Sciences, Wyeth Research, Collegeville, Pennsylvania 19426, USA. [email protected]
PMID: 19072540 DOI: 10.1021/jm801144h
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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