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https://repository.monashhealth.org/monashhealthjspui/handle/1/30321| Title: | 2-Phenyl and 2-heterocyclic-4-(3-(pyridin-2-yl)-1H-pyrazol-4-yl)pyridines as inhibitors of TGF-beta1 and activin A signalling. | Authors: | Harrison C.A.;Hearn M.T.W.;Walton K.L.;Kelso G.F.;Harris S.J.;Ciayadi R.;Potdar M. | 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, Australia | Issue Date: | 5-Oct-2012 | Copyright year: | 2011 | Publisher: | Elsevier Ltd (Langford Lane, Kidlington, Oxford OX5 1GB, United Kingdom) | Place of publication: | United Kingdom | Publication information: | Bioorganic and Medicinal Chemistry Letters. 21 (18) (pp 5642-5645), 2011. Date of Publication: 15 Sep 2011. | Abstract: | Novel 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. | DOI: | http://monash.idm.oclc.org/login?url=http://dx.doi.org/10.1016/j.bmcl.2010.12.120 | PubMed URL: | 21783359 [http://www.ncbi.nlm.nih.gov/pubmed/?term=21783359] | ISSN: | 0960-894X | URI: | https://repository.monashhealth.org/monashhealthjspui/handle/1/30321 | Type: | Article |
| Appears in Collections: | Articles |
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