Aseries of structurally related mono-and bis-NHC–iridium(I) (NHC:N-heterocyclic carbene) complexeshave been investigatedfor their suitability as potential anti-cancer drugs.Their spectral behaviour in aqueous buffersunder physiologic al-like conditions and their cytotoxicityagainstthe cancercell lines MCF-7 and HT-29are reported.Notably,almostall complexes exhibit significant cytotoxic ef-fects towards both cancer cell lines. In general,the cationicbis-carbene complex es show higherstabilityand greater an-ticanceractivity than their neutral mono-carbene analogueswith IC50valuesinthe high nanomolar range.Furthermore,to gain initialmechanistic insight, the interactions of theseiridium(I)–NHC complexes with two model proteins,namelylysozyme and cytochrome c, were exploredbyHR-ESI-MSanalyses. The different protein metalation patternsofthecomplexes can be roughlyclassified into two distinctgroups. Those interactions give us afirst idea about the pos-sible mechanism of action of this class of compounds. Over-all, our findings show that iridium(I)–NHC complexesrepre-sent very interesting candidates forfurther development asnew metal-based anticancer drugs.
Iridium(I) Compounds as Prospective Anticancer Agents: Solution Chemistry, Antiproliferative Profiles and Protein Interactions for a Series of Iridium(I) N-Heterocyclic Carbene Complexes / Gothe, Yvonne; Marzo, Tiziano; Messori, Luigi; Metzler-Nolte, Nils. - In: CHEMISTRY-A EUROPEAN JOURNAL. - ISSN 0947-6539. - ELETTRONICO. - 22:(2016), pp. 12487-12494. [10.1002/chem.201601542]
Iridium(I) Compounds as Prospective Anticancer Agents: Solution Chemistry, Antiproliferative Profiles and Protein Interactions for a Series of Iridium(I) N-Heterocyclic Carbene Complexes
MARZO, TIZIANO;MESSORI, LUIGI;
2016
Abstract
Aseries of structurally related mono-and bis-NHC–iridium(I) (NHC:N-heterocyclic carbene) complexeshave been investigatedfor their suitability as potential anti-cancer drugs.Their spectral behaviour in aqueous buffersunder physiologic al-like conditions and their cytotoxicityagainstthe cancercell lines MCF-7 and HT-29are reported.Notably,almostall complexes exhibit significant cytotoxic ef-fects towards both cancer cell lines. In general,the cationicbis-carbene complex es show higherstabilityand greater an-ticanceractivity than their neutral mono-carbene analogueswith IC50valuesinthe high nanomolar range.Furthermore,to gain initialmechanistic insight, the interactions of theseiridium(I)–NHC complexes with two model proteins,namelylysozyme and cytochrome c, were exploredbyHR-ESI-MSanalyses. The different protein metalation patternsofthecomplexes can be roughlyclassified into two distinctgroups. Those interactions give us afirst idea about the pos-sible mechanism of action of this class of compounds. Over-all, our findings show that iridium(I)–NHC complexesrepre-sent very interesting candidates forfurther development asnew metal-based anticancer drugs.File | Dimensione | Formato | |
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