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. 2016 Feb 15;26(4):1184-7.
doi: 10.1016/j.bmcl.2016.01.038. Epub 2016 Jan 18.

4H-Thieno[3,2-c]chromene based inhibitors of Notum Pectinacetylesterase

Qiang Han  1 , Praveen K Pabba  1 , Joseph Barbosa  1 , Ross Mabon  1 , Jason P Healy  1 , Michael W Gardyan  1 , Kristen M Terranova  1 , Robert Brommage  2 , Andrea Y Thompson  2 , James M Schmidt  2 , Alan G E Wilson  2 , Xiaolian Xu  1 , James E Tarver Jr  3 , Kenneth G Carson  1
Affiliations

4H-Thieno[3,2-c]chromene based inhibitors of Notum Pectinacetylesterase

Qiang Han et al. Bioorg Med Chem Lett. .

Abstract

A group of small molecule thienochromenes inhibitors of Notum Pectinacetylesterase are described. We developed SAR on three series based on carbon, oxygen and sulfur replacement of the 5-position. In each series, highly potent Notum Pectinacetylesterase inhibitors were identified.

Keywords: Femur cortical bone thickness; Notum Pectinacetylesterase; Osteroporosis; SAR; Thienochromene.

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