Please use this identifier to cite or link to this item:
https://hdl.handle.net/2440/42095
Citations | ||
Scopus | Web of Science® | Altmetric |
---|---|---|
?
|
?
|
Type: | Journal article |
Title: | Evaluation of 4'-substituted bicyclic pyridones as non-steroidal inhibitors of steroid 5a-reductase |
Author: | McCarthy, A. Hartmann, R. Abell, A. |
Citation: | Bioorganic and Medicinal Chemistry Letters, 2007; 17(13):3603-3607 |
Publisher: | Pergamon-Elsevier Science Ltd |
Issue Date: | 2007 |
ISSN: | 0960-894X 1464-3405 |
Statement of Responsibility: | Anna R. McCarthy, Rolf W. Hartmann and Andrew D. Abell |
Abstract: | 4′-Substituted bicyclic pyridones were prepared and evaluated as non-steroidal inhibitors of type 1 and 2 steroid 5greek small letter alpha-reductase (SR). A range of 4′-substituents were incorporated into the bicyclic scaffold to investigate SAR within and across different classes of non-steroidal inhibitors of SR. Bicyclic pyridones containing a 4′-benzoyl or long carbon chain tether showed more potent inhibition against type 1 SR than inhibitors with N-substituted acetamide groups in the 4′-position. SAR derived from 4′-substituted bicyclic pyridones reported here do not correlate with SAR derived from known potent 4′-substituted biaryl acid SR inhibitors. A 4′-benzoyl group is favoured by the active site in both isozymes. |
Keywords: | Kidney Cell Line Humans Carbon Pyridones Steroids Protein Isoforms Enzyme Inhibitors Inhibitory Concentration 50 Binding Sites Structure-Activity Relationship Drug Design Chemistry, Pharmaceutical Models, Chemical 3-Oxo-5-alpha-Steroid 4-Dehydrogenase 5-alpha Reductase Inhibitors |
DOI: | 10.1016/j.bmcl.2007.04.049 |
Published version: | http://dx.doi.org/10.1016/j.bmcl.2007.04.049 |
Appears in Collections: | Aurora harvest Chemistry and Physics publications |
Files in This Item:
There are no files associated with this item.
Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.