The synthesis of 4,6-diaryl-2-pyridones and their bioactivation in CYP1 expressing breast cancer cells

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dc.cclicenceCC-BY-NC-NDen
dc.contributor.authorLodhi, Sabahat
dc.contributor.authorAnkrett, Dyan N.
dc.contributor.authorWilsher, Nicola E.
dc.contributor.authorPotter, Gerard A.
dc.contributor.authorBeresford, Kenneth J. M.
dc.contributor.authorArroo, R. R. J.
dc.contributor.authorRuparelia, K. C.
dc.date.acceptance2019-03-22
dc.date.accessioned2019-04-02T10:16:14Z
dc.date.available2019-04-02T10:16:14Z
dc.date.issued2019-03-22
dc.descriptionThe file attached to this record is the author's final peer reviewed version. The Publisher's final version can be found by following the DOI link.en
dc.description.abstractAs part of a programme to develop anticancer prodrugs which are activated by cytochrome P450 (CYP)1B1, a library of 4,6-diaryl-2-pyridones was synthesised in yields of 6-60% from the corresponding chalcones. A number of these derivatives showed promising antiproliferative activities in human breast cancer cell lines which express CYP1B1 and CYP1A1, while showing little toxicity towards a non-tumour breast cell line with no CYP expression. Metabolism studies provided evidence supporting the involvement of CYP1 enzymes in the bioactivation of these compounds.en
dc.funderEPSRC (Engineering and Physical Sciences Research Council)en
dc.identifier.citationRuparelia, K.C., Lodhi, S., Ankrett, D.N., Wilsher, N.E., Arroo, R.R.J., Potter, G.A., Beresford, K.J.M. (2019) The synthesis of 4,6-diaryl-2-pyridones and their bioactivation in CYP1 expressing breast cancer cells. Bioorganic & Medicinal Chemistry Letters, 29 (11), pp. 1403-1406en
dc.identifier.doihttps://doi.org/10.1016/j.bmcl.2019.03.030
dc.identifier.issn0960-894X
dc.identifier.urihttps://www.dora.dmu.ac.uk/handle/2086/17673
dc.language.isoenen
dc.peerreviewedYesen
dc.projectidN/Aen
dc.publisherElsevieren
dc.researchinstituteLeicester Institute for Pharmaceutical Innovation - From Molecules to Practice (LIPI)en
dc.subject4,6-diaryl-2-pyridonesen
dc.subjectchalconesen
dc.subjectantiproliferativeen
dc.subjectprodrugen
dc.subjectCYP1B1en
dc.titleThe synthesis of 4,6-diaryl-2-pyridones and their bioactivation in CYP1 expressing breast cancer cellsen
dc.typeArticleen

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