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dc.contributor.authorRuparelia, K. C.en
dc.contributor.authorLjaza, T.en
dc.contributor.authorAnkrett, D. N.en
dc.contributor.authorWilsher, Nicola Elizabethen
dc.contributor.authorLodhia, S.en
dc.contributor.authorBeresford, Kenneth J. M.en
dc.contributor.authorBhambra, Avninder S.en
dc.contributor.authorArroo, R. R. J.en
dc.contributor.authorPotter, G. A.en
dc.contributor.authorButler, P. C.en
dc.contributor.authorTan, Hoon Leongen
dc.contributor.authorZeka, K.en
dc.date.accessioned2018-03-05T12:22:13Z
dc.date.available2018-03-05T12:22:13Z
dc.date.issued2017-12-11
dc.identifier.citationRuparelia, K.C. et al. (2017) The synthesis of chalcones as anticancer prodrugs and their bioactivation in CYP1 expressing breast cancer cells. Medicinal Chemistry, 14 (4), pp. 322-332en
dc.identifier.issn1573-4064
dc.identifier.urihttp://hdl.handle.net/2086/15336
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 linken
dc.description.abstractAbstract: Background: Although the expression levels of many P450s differ between tumour and corresponding normal tissue, CYP1B1 is one of the few CYP subfamilies which is significantly and consistently overexpressed in tumours. CYP1B1 has been shown to be active within tumours and is capable of metabolising a structurally diverse range of anticancer drugs. Because of this, and its role in the activation of procarcinogens, CYP1B1 is seen as an important target for anticancer drug development. Objectives: To synthesise a series of chalcone derivatives based on the chemopreventative agent DMU-135 and investigate their antiproliferative activities in human breast cancer cell lines which express CYP1B1 and CYP1A1. Method: A series of chalcones were synthesised in yields of 43-94% using the Claisen-Schmidt condensation reaction. These were screened using a MTT assay against a panel of breast cancer cell lines which have been characterised for CYP1 expression. Results: A number of derivatives showed promising antiproliferative activities in human breast cancer cell lines which express CYP1B1 and CYP1A1, while showing significantly lower toxicity towards a non-tumour breast cell line with no CYP expression. Experiments using the CYP1 inhibitors acacetin and 􀀁-naphthoflavone provided supporting evidence for the involvement of CYP1 enzymes in the bioactivation of these compounds. Conclusions: Chalcones show promise as anticancer agents with evidence suggesting that CYP1 activation of these compounds may be involved.en
dc.language.isoenen
dc.publisherBentham Science Publishersen
dc.subjectAntiproliferativeen
dc.subjectcanceren
dc.subjectchalconesen
dc.subjectCYP1A1en
dc.subjectCYP1B1en
dc.subjectprodrugen
dc.titleThe synthesis of chalcones as anticancer prodrugs and their bioactivation in CYP1 expressing breast cancer cellsen
dc.typeArticleen
dc.identifier.doihttps://doi.org/10.2174/1573406414666180112120134
dc.researchgroupChemistry for Healthen
dc.peerreviewedYesen
dc.funderN/Aen
dc.projectidN/Aen
dc.cclicenceCC-BY-NCen
dc.date.acceptance2017-12-11en
dc.researchinstituteInstitute for Allied Health Sciences Researchen


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