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Organometallic Ru, Os, Rh and Ir half-sandwich conjugates of ispinesib – impact of the organometallic group on the antimitotic activity

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dc.abstract.enAntimitotic agents are among the most important drugs used in anticancer therapy. Kinesin spindle protein (KSP) was proposed as a promising target for new antimitotic drugs. Herein, we report the syn-thesis of Ru, Os, Rh, and Ir half-sandwich complexes with the KSP inhibitor ispinesib and its (S)-enantio- mer. Conjugation of the organometallic moiety with ispinesib and its (S)-enantiomer resulted in a signifi- cantly increased cytotoxicity of up to 5.6-fold compared to the parent compounds, with IC 50 values in the nanomolar range. The most active derivatives were the ispinesib Ru and Rh conjugates which were able to generate reactive oxygen species (ROS), which may at least partially explain their high cytotoxicity. At the same time, the Os and Ir derivatives acted as KSP inhibitors with no effects on ROS generation
dc.affiliationUniwersytet Warszawski
dc.contributor.authorPlażuk, Damian
dc.contributor.authorRychlik, Błażej
dc.contributor.authorHartinger, Christian
dc.contributor.authorAyine-Tora, Daniel Moscoh
dc.contributor.authorTchoń, Daniel
dc.contributor.authorMakal, Anna
dc.contributor.authorGłodek, Marta
dc.contributor.authorBłauż, Andrzej
dc.contributor.authorŁomzik, Michał
dc.date.accessioned2024-01-25T16:09:22Z
dc.date.available2024-01-25T16:09:22Z
dc.date.issued2023
dc.description.financeNie dotyczy
dc.identifier.doi10.1039/D3DT01217D
dc.identifier.issn1477-9226
dc.identifier.urihttps://repozytorium.uw.edu.pl//handle/item/115059
dc.identifier.weblinkhttp://pubs.rsc.org/en/content/articlepdf/2023/DT/D3DT01217D
dc.languageeng
dc.pbn.affiliationchemical sciences
dc.relation.ispartofDalton Transactions
dc.rightsClosedAccess
dc.sciencecloudnosend
dc.titleOrganometallic Ru, Os, Rh and Ir half-sandwich conjugates of ispinesib – impact of the organometallic group on the antimitotic activity
dc.typeJournalArticle
dspace.entity.typePublication