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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 & Medicinal Chemistry Letters, 2007; 17(13):3603-3607
Publisher: Pergamon-Elsevier Science Ltd
Issue Date: 2007
ISSN: 0960-894X
Statement of
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
RMID: 0020075683
DOI: 10.1016/j.bmcl.2007.04.049
Appears in Collections:Chemistry and Physics publications

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