Synthesis of steroidal inhibitors for Mycobacterium tuberculosis

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dc.contributor.authorChurchman, L.R.
dc.contributor.authorBeckett, J.R.
dc.contributor.authorTan, L.
dc.contributor.authorWoods, K.
dc.contributor.authorDoherty, D.Z.
dc.contributor.authorGhith, A.
dc.contributor.authorBernhardt, P.V.
dc.contributor.authorBell, S.G.
dc.contributor.authorWest, N.P.
dc.contributor.authorDe Voss, J.J.
dc.date.issued2024
dc.descriptionAvailable online 10 February 2024
dc.description.abstractOxidised derivatives of cholesterol have been shown to inhibit the growth of Mycobacterium tuberculosis (Mtb). The bacteriostatic activity of these compounds has been attributed to their inhibition of CYP125A1 and CYP142A1, two metabolically critical cytochromes P450 that initiate degradation of the sterol side chain. Here, we synthesise and characterise an extensive library of 28 cholesterol derivatives to develop a structure-activity relationship for this class of inhibitors. The candidate compounds were evaluated for MIC with virulent Mtb and in binding studies with CYP125A1 and CYP142A1 from Mtb.
dc.description.statementofresponsibilityLuke R. Churchman, James R. Beckett, Lendl Tan, Kyra Woods, Daniel Z. Doherty, Amna Ghith, Paul V. Bernhardt, Stephen G. Bell, Nicholas P. West, James J. De Voss
dc.identifier.citationJournal of Steroid Biochemistry and Molecular Biology, 2024; 239:106479-1-106479-16
dc.identifier.doi10.1016/j.jsbmb.2024.106479
dc.identifier.issn0960-0760
dc.identifier.issn1879-1220
dc.identifier.orcidGhith, A. [0000-0003-1753-6939]
dc.identifier.orcidBell, S.G. [0000-0002-7457-9727]
dc.identifier.urihttps://hdl.handle.net/2440/140697
dc.language.isoen
dc.publisherElsevier
dc.relation.granthttp://purl.org/au-research/grants/arc/DP210103970
dc.rights© 2024 Published by Elsevier Ltd.
dc.source.urihttp://dx.doi.org/10.1016/j.jsbmb.2024.106479
dc.subjectCholesterol
dc.subjectCytochrome P450
dc.subjectInhibition
dc.subjectSteroid
dc.subjectTuberculosis
dc.titleSynthesis of steroidal inhibitors for Mycobacterium tuberculosis
dc.typeJournal article
pubs.publication-statusPublished

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