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Please use this identifier to cite or link to this item: https://repository.monashhealth.org/monashhealthjspui/handle/1/30321
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dc.contributor.authorHarrison C.A.en
dc.contributor.authorHearn M.T.W.en
dc.contributor.authorWalton K.L.en
dc.contributor.authorKelso G.F.en
dc.contributor.authorHarris S.J.en
dc.contributor.authorCiayadi R.en
dc.contributor.authorPotdar M.en
dc.date.accessioned2021-05-14T10:14:55Zen
dc.date.available2021-05-14T10:14:55Zen
dc.date.copyright2011en
dc.date.created20110901en
dc.date.issued2012-10-05en
dc.identifier.citationBioorganic and Medicinal Chemistry Letters. 21 (18) (pp 5642-5645), 2011. Date of Publication: 15 Sep 2011.en
dc.identifier.issn0960-894Xen
dc.identifier.urihttps://repository.monashhealth.org/monashhealthjspui/handle/1/30321en
dc.description.abstractNovel inhibitors of TGF-beta1 and activin A signalling based on a 2-aryl-4-(3-(pyridin-2-yl)-1H-pyrazol-4-yl)pyridine pharmacophore have been synthesised. Compounds containing phenyl or aromatic nitrogen heterocycle substituents inhibited both types of signalling with HEK-293T cells in culture, with a selectivity preference for TGF-beta1. Synthetic compounds containing pyridin-3-yl, pyrazol-4-yl, pyrazol-1-yl or 1H-imidazoyl-1-yl substituents exhibited structural and functional attributes suitable for further investigation related to the development of more potent TGF-beta inhibitors. © 2011 Elsevier Ltd. All rights reserved.en
dc.languageEnglishen
dc.languageenen
dc.publisherElsevier Ltd (Langford Lane, Kidlington, Oxford OX5 1GB, United Kingdom)en
dc.title2-Phenyl and 2-heterocyclic-4-(3-(pyridin-2-yl)-1H-pyrazol-4-yl)pyridines as inhibitors of TGF-beta1 and activin A signalling.en
dc.typeArticleen
dc.identifier.doihttp://monash.idm.oclc.org/login?url=http://dx.doi.org/10.1016/j.bmcl.2010.12.120en
dc.publisher.placeUnited Kingdomen
dc.identifier.pubmedid21783359 [http://www.ncbi.nlm.nih.gov/pubmed/?term=21783359]en
dc.identifier.source51534723en
dc.identifier.institution(Ciayadi, Potdar, Kelso, Harris, Hearn) Centre for Green Chemistry, Monash University, Clayton, VIC 3800, Australia (Walton, Harrison) Prince Henry's Institute, Monash Medical Centre, Clayton, VIC 3168, Australiaen
dc.description.addressM.T.W. Hearn, Centre for Green Chemistry, Monash University, Clayton, VIC 3800, Australia. E-mail: milton.hearn@monash.eduen
dc.description.publicationstatusEmbaseen
dc.rights.statementCopyright 2012 Elsevier B.V., All rights reserved.en
dc.subect.keywordsActivin A ATP-competitive ALK4/ALK5 inhibitors Low molecular weight inhibitors Structure-activity relationships Transforming growth factor-betaen
dc.identifier.authoremailHearn M.T.W.; milton.hearn@monash.eduen
item.fulltextNo Fulltext-
item.cerifentitytypePublications-
item.grantfulltextnone-
item.openairetypeArticle-
item.openairecristypehttp://purl.org/coar/resource_type/c_18cf-
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