Stimulation of cortical bone formation with thienopyrimidine based inhibitors of Notum Pectinacetylesterase

  • Bioorg Med Chem Lett. 2016 Mar 15;26(6):1525-1528. doi: 10.1016/j.bmcl.2016.02.021.
James E Tarver Jr  1 ,  Praveen K Pabba  2 ,  Joseph Barbosa  2 ,  Qiang Han  2 ,  Michael W Gardyan  2 ,  Robert Brommage  3 ,  Andrea Y Thompson  3 ,  James M Schmidt  3 ,  Alan G E Wilson  3 ,  Wei He  2 ,  Victoria K Lombardo  2 ,  Kenneth G Carson  2
Affiliations
  • 1. Lexicon Pharmaceuticals, 350 Carter Road, Princeton, NJ 08540, United States. Electronic address: [email protected].
  • 2. Lexicon Pharmaceuticals, 350 Carter Road, Princeton, NJ 08540, United States.
  • 3. Lexicon Pharmaceuticals, 8800 Technology Forest Place, The Woodlands, TX 77381, United States.
PMID: 26897593 DOI: 10.1016/j.bmcl.2016.02.021
Abstract

A group of small molecule thienopyrimidine inhibitors of Notum Pectinacetylesterase are described. We explored both 2-((5,6-thieno[2,3-d]pyrimidin-4-yl)thio)acetic acids and 2-((6,7-thieno[3,2-d]pyrimidin-4-yl)thio)acetic acids. In both series, highly potent, orally active Notum Pectinacetylesterase inhibitors were identified.

Keywords
Femur cortical bone thickness; Notum Pectinacetylesterase; Osteoporosis; SAR; Thienopyrimidine.
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-131034
    LP-922056
    99.63%, Notum Pectinacetylesterase Inhibitor
    target: Wnt
    Research Areas: Others