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Artemisinin-polypyrrole conjugates: synthesis, DNA binding studies and preliminary antiproliferative evaluation

2013Journal article Restricted access
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dc.contributor.authorLa Pensée, Louise
dc.contributor.authorSabbani, Sunil
dc.contributor.authorSharma, Raman
dc.contributor.authorBhamra, Inder
dc.contributor.authorShore, Emma
dc.contributor.authorChadwick, Amy E.
dc.contributor.authorBerry, Neil
dc.contributor.authorFirman, J.
dc.contributor.authorAraujo, Nuna C. P.
dc.contributor.authorCabral, Lília
dc.contributor.authorCristiano, Maria Lurdes Santos
dc.contributor.authorBateman, Cerys
dc.contributor.authorJanneh, Omar
dc.contributor.authorGavrila, Adelina
dc.contributor.authorWu, Yi Hang
dc.contributor.authorHussain, Afthab
dc.contributor.authorWard, Stephen A.
dc.contributor.authorStocks, Paul A.
dc.contributor.authorCosstick, Rick
dc.contributor.authorO'Neill, Paul M.
dc.date.accessioned2014-06-06T15:58:40Z
dc.date.available2014-06-06T15:58:40Z
dc.date.issued2013
dc.date.updated2014-05-30T15:17:19Z
dc.description.abstractArtemisinin-based combination therapies (ACTs) are currently the recommended treatment for uncomplicated and severe cases of malaria.[1] Additionally, artemisinins, as well as a number of other sesquiterpene lactones (SLs), are currently in phase I–II clinical trials against breast, colorectal and nonsmall-cell lung cancers.[2] As outlined by the iron-dependent activation hypothesis,[3] the activity of artemisinin (ART) is dependent on the endoperoxide bridge.[4] The peroxide is cleaved by endogenous sources of FeII to generate highly reactive carbon-centred radicals (CCRs), which are believed to react with critical cellular targets.[3] ART demonstrates selectivity towards rapidly proliferating cancer cell lines that possess a high intracellular iron content required to sustain their characteristic high rates of multiplication.[5] Iron activation links this particular potency of ART towards rapidly proliferating cancer cell lines; differentiation between healthy and cancerous cells by variation of iron concentration provides a strategy for selective cytotoxicity by ART and its derivatives.[4] The mechanism by which ART exerts its cytotoxic activity still remains elusive. ART acts by disruption of proliferation,[6, 7] oxidative stress,[8] anti-angiogenesis,[9] NF-kB signalling,[10] apoptosis[4] and interfering with iron uptake and metabolism.[6] ART also induces DNA breakage,[11] and it has been reported that artesunate-mediated DNA damage contributes to its therapeutic efficacy.por
dc.identifier.citationLa Pensée, Louise; Sabbani, Sunil; Sharma, Raman; Bhamra, Inder; Shore, Emma; Chadwick, Amy E.; Berry, Neil G.; Firman, James; Araujo, Nuna C.; Cabral, Lília; Cristiano, Maria L. S.; Bateman, Cerys; Janneh, Omar; Gavrila, Adelina; Wu, Yi Hang; Hussain, Afthab; Ward, Stephen A.; Stocks, Paul A.; Cosstick, Rick; O’Neill, Paul M. Artemisinin-Polypyrrole Conjugates: Synthesis, DNA Binding Studies and Preliminary Antiproliferative Evaluation, ChemMedChem, 8, 5, 709-718, 2013.por
dc.identifier.doihttp://dx.doi.org/10.1002/cmdc.201200536
dc.identifier.issn1860-7179
dc.identifier.otherAUT: MCR00716;
dc.identifier.urihttp://hdl.handle.net/10400.1/4230
dc.language.isoengpor
dc.peerreviewedyespor
dc.publisherWileypor
dc.subjectArtemisininpor
dc.subjectMolecular modellingpor
dc.subjectDNApor
dc.subjectCytotoxicitypor
dc.subjectBinding studiespor
dc.titleArtemisinin-polypyrrole conjugates: synthesis, DNA binding studies and preliminary antiproliferative evaluationpor
dc.typejournal article
dspace.entity.typePublication
oaire.citation.endPage718por
oaire.citation.issue5por
oaire.citation.startPage709por
oaire.citation.titleChemMedChempor
oaire.citation.volume8por
person.familyNameAraujo
person.familyNameCabral
person.familyNameCristiano
person.givenNameNuna
person.givenNameLília
person.givenNameMaria de Lurdes
person.identifier.ciencia-id3510-24A8-36B6
person.identifier.ciencia-idE411-6006-5A01
person.identifier.orcid0000-0002-7602-0150
person.identifier.orcid0000-0001-9362-8128
person.identifier.orcid0000-0002-9447-2855
person.identifier.ridN-8531-2013
person.identifier.ridM-4279-2013
person.identifier.ridG-2345-2012
person.identifier.scopus-author-id9238724800
rcaap.rightsrestrictedAccesspor
rcaap.typearticlepor
relation.isAuthorOfPublication3423e71b-934d-4da7-9c81-4e56c7930252
relation.isAuthorOfPublication175a6aa3-9993-480b-9663-ed083a17eedf
relation.isAuthorOfPublicationb16751a6-748e-44b0-9c59-058cbd5b2cc3
relation.isAuthorOfPublication.latestForDiscovery3423e71b-934d-4da7-9c81-4e56c7930252

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