Please use this identifier to cite or link to this item: https://hdl.handle.net/2440/42095
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dc.contributor.authorMcCarthy, A.en
dc.contributor.authorHartmann, R.en
dc.contributor.authorAbell, A.en
dc.date.issued2007en
dc.identifier.citationBioorganic & Medicinal Chemistry Letters, 2007; 17(13):3603-3607en
dc.identifier.issn0960-894Xen
dc.identifier.issn1464-3405en
dc.identifier.urihttp://hdl.handle.net/2440/42095-
dc.description.abstract4′-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.en
dc.description.statementofresponsibilityAnna R. McCarthy, Rolf W. Hartmann and Andrew D. Abellen
dc.language.isoenen
dc.publisherPergamon-Elsevier Science Ltden
dc.subjectKidney; 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 Inhibitorsen
dc.titleEvaluation of 4'-substituted bicyclic pyridones as non-steroidal inhibitors of steroid 5a-reductaseen
dc.typeJournal articleen
dc.identifier.doi10.1016/j.bmcl.2007.04.049en
pubs.publication-statusPublisheden
dc.identifier.orcidAbell, A. [0000-0002-0604-2629]en
Appears in Collections:Chemistry and Physics publications

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