1.
Bioorg Med Chem Lett
; 26(6): 1525-1528, 2016 Mar 15.
Article
in English
| MEDLINE
| ID: mdl-26897593
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.
Subject(s)
Enzyme Inhibitors/pharmacology , Esterases/antagonists & inhibitors , Femur/drug effects , Osteogenesis/drug effects , Pyrimidines/pharmacology , Animals , Dose-Response Relationship, Drug , Enzyme Inhibitors/chemical synthesis , Enzyme Inhibitors/chemistry , Esterases/metabolism , Femur/anatomy & histology , Femur/growth & development , Humans , Mice , Molecular Structure , Pyrimidines/chemical synthesis , Pyrimidines/chemistry , Structure-Activity Relationship
2.
Bioorg Med Chem Lett
; 26(4): 1184-7, 2016 Feb 15.
Article
in English
| MEDLINE
| ID: mdl-26821819
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.
