2. Academic Validation
  3. Stimulation of cortical bone formation with thienopyrimidine based inhibitors of Notum Pectinacetylesterase

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

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.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-131034
    98.08%, Notum Pectinacetylesterase Inhibitor
    Wnt