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4H-Thieno[3,2-c]chromene based inhibitors of Notum Pectinacetylesterase
- Source :
- Bioorganic & Medicinal Chemistry Letters. 26:1184-1187
- Publication Year :
- 2016
- Publisher :
- Elsevier BV, 2016.
-
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.
- Subjects :
- Male
0301 basic medicine
animal structures
Stereochemistry
Clinical Biochemistry
Pharmaceutical Science
Biochemistry
Inhibitory Concentration 50
Mice
Structure-Activity Relationship
03 medical and health sciences
0302 clinical medicine
Drug Discovery
Animals
Humans
Benzopyrans
Femur
Enzyme Inhibitors
Molecular Biology
Chemistry
fungi
Organic Chemistry
Esterases
Small molecule
Notum
030104 developmental biology
Pectinacetylesterase
030220 oncology & carcinogenesis
embryonic structures
Osteoporosis
Molecular Medicine
Half-Life
Protein Binding
Subjects
Details
- ISSN :
- 0960894X
- Volume :
- 26
- Database :
- OpenAIRE
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Accession number :
- edsair.doi.dedup.....990401977cc295fc807cd6291e6f9d8d
- Full Text :
- https://doi.org/10.1016/j.bmcl.2016.01.038