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dc.contributor.authorChoomuenwai, Vanida
dc.contributor.authorAndrews, Katherine T
dc.contributor.authorDavis, Rohan A
dc.date.accessioned2017-05-03T11:45:17Z
dc.date.available2017-05-03T11:45:17Z
dc.date.issued2012
dc.date.modified2014-02-06T01:40:21Z
dc.identifier.issn0968-0896
dc.identifier.doi10.1016/j.bmc.2012.09.052
dc.identifier.urihttp://hdl.handle.net/10072/51656
dc.description.abstractAs part of a research program aimed at discovering new antimalarial leads from Australian macrofungi a unique fungi-derived prefractionated library was screened against a chloroquine-sensitive Plasmodium falciparum line (3D7) using a radiometric growth inhibition assay. A library fraction derived from a Cortinarius species displayed promising antimalarial activity. UV-guided fractionation on the CH2Cl2/MeOH extract from this fungus resulted in the isolation of four known compounds: (1S,3R)-austrocortirubin (1), (1S,3S)-austrocortirubin (2), 1-deoxyaustrocortirubin (3), and austrocortinin (4). Compound 2 was used as a natural product scaffold in the parallel solution-phase synthesis of a small library of N-substituted tetrahydroanthraquinones (5-15). All compounds (1-15) were tested in vitro against P. falciparum 3D7 parasites and (1S,3S)-austrocortirubin (2), the major fungal constituent, was shown to be the most active compound with an IC50 of 1.9 卮 This compound displayed moderate cytotoxicity against neonatal foreskin fibroblast (NFF) cells with an IC50 of 15.6 卮
dc.description.peerreviewedYes
dc.description.publicationstatusYes
dc.format.extent493541 bytes
dc.format.mimetypeapplication/pdf
dc.languageEnglish
dc.language.isoeng
dc.publisherElsevier
dc.publisher.placeNetherlands
dc.relation.ispartofstudentpublicationY
dc.relation.ispartofpagefrom7167
dc.relation.ispartofpageto7174
dc.relation.ispartofissue24
dc.relation.ispartofjournalBioorganic & Medicinal Chemistry
dc.relation.ispartofvolume20
dc.rights.retentionY
dc.subject.fieldofresearchMedicinal and biomolecular chemistry
dc.subject.fieldofresearchOrganic chemistry
dc.subject.fieldofresearchInfectious agents
dc.subject.fieldofresearchPharmacology and pharmaceutical sciences
dc.subject.fieldofresearchBiochemistry and cell biology
dc.subject.fieldofresearchcode3404
dc.subject.fieldofresearchcode3405
dc.subject.fieldofresearchcode310702
dc.subject.fieldofresearchcode3214
dc.subject.fieldofresearchcode3101
dc.titleSynthesis and antimalarial evaluation of a screening library based on a tetrahydroanthraquinone natural product scaffold
dc.typeJournal article
dc.type.descriptionC1 - Articles
dc.type.codeC - Journal Articles
gro.facultyGriffith Sciences, Griffith Institute for Drug Discovery
gro.rights.copyright© 2012 Elsevier. This is the author-manuscript version of this paper. Reproduced in accordance with the copyright policy of the publisher. Please refer to the journal's website for access to the definitive, published version.
gro.date.issued2012
gro.hasfulltextFull Text
gro.griffith.authorAndrews, Katherine T.
gro.griffith.authorDavis, Rohan A.


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