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

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

Affiliation

  • 1 Chemical and Screening Sciences, Wyeth Research, Collegeville, Pennsylvania 19426, USA. moorew2@wyeth.com
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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