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dc.contributor.authorChellan, Prinessa
dc.contributor.authorAvery, Vicky M
dc.contributor.authorDuffy, Sandra
dc.contributor.authorLand, Kirkwood M
dc.contributor.authorTam, Christina C
dc.contributor.authorKim, Jong H
dc.contributor.authorCheng, Luisa W
dc.contributor.authorRomero-Canelón, Isolda
dc.contributor.authorSadler, Peter J
dc.date.accessioned2021-04-14T05:21:15Z
dc.date.available2021-04-14T05:21:15Z
dc.date.issued2021
dc.identifier.issn0162-0134
dc.identifier.doi10.1016/j.jinorgbio.2021.111408
dc.identifier.urihttp://hdl.handle.net/10072/403747
dc.description.abstractReaction of dihydroartemisinin (DHA) with 4-methyl-4′-carboxy-2,2′-bipyridine yielded the new ester derivative L1. Six novel organometallic half-sandwich chlorido Rh(III) and Ir(III) complexes (1–6) containing pentamethylcyclopentadienyl, (Cp*), tetramethylphenylcyclopentadienyl (Cpxph), or tetramethylbiphenylcyclopentadienyl (Cpxbiph), and N,N-chelated bipyridyl group of L1, have been synthesized and characterized. The complexes were screened for inhibitory activity against the Plasmodium falciparum 3D7 (sensitive), Dd2 (multi-drug resistant) and NF54 late stage gametocytes (LSGNF54), the parasite strain Trichomonas vaginalis G3, as well as A2780 (human ovarian carcinoma), A549 (human alveolar adenocarcinoma), HCT116 (human colorectal carcinoma), MCF7 (human breast cancer) and PC3 (human prostate cancer) cancer cell lines. They show nanomolar antiplasmodial activity, outperforming chloroquine and artemisinin. Their activities were also comparable to dihydroartemisinin. As anticancer agents, several of the complexes showed high inhibitory effects, with Ir(III) complex 3, containing the tetramethylbiphenylcyclopentadienyl ligand, having similar IC50 values (concentration for 50% of maximum inhibition of cell growth) as the clinical drug cisplatin (1.06–9.23 μM versus 0.24–7.2 μM, respectively). Overall, the iridium complexes (1–3) are more potent compared to the rhodium derivatives (4–6), and complex 3 emerges as the most promising candidate for future studies.
dc.description.peerreviewedYes
dc.languageen
dc.publisherElsevier BV
dc.relation.ispartofpagefrom111408
dc.relation.ispartofjournalJournal of Inorganic Biochemistry
dc.relation.ispartofvolume219
dc.relation.urihttp://purl.org/au-research/grants/NHMRC/GNT1150359
dc.relation.grantIDGNT1150359
dc.relation.fundersNHMRC
dc.subject.fieldofresearchInorganic chemistry
dc.subject.fieldofresearchTheoretical and computational chemistry
dc.subject.fieldofresearchOther chemical sciences
dc.subject.fieldofresearchcode3402
dc.subject.fieldofresearchcode3407
dc.subject.fieldofresearchcode3499
dc.titleBioactive half-sandwich Rh and Ir bipyridyl complexes containing artemisinin
dc.typeJournal article
dc.type.descriptionC1 - Articles
dcterms.bibliographicCitationChellan, P; Avery, VM; Duffy, S; Land, KM; Tam, CC; Kim, JH; Cheng, LW; Romero-Canelón, I; Sadler, PJ, Bioactive half-sandwich Rh and Ir bipyridyl complexes containing artemisinin, Journal of Inorganic Biochemistry, 2021, 219, pp. 111408
dc.date.updated2021-04-14T03:15:37Z
gro.hasfulltextNo Full Text
gro.griffith.authorAvery, Vicky M.
gro.griffith.authorDuffy, Sandra


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