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Cytotoxic hydrogen bridged ruthenium quinaldamide complexes showing induced cancer cell death by apoptosis

Yes / This report presents the first known p-cymene ruthenium quinaldamide complexes which are stabilised
by a hydrogen-bridging atom, [{(p-cym)RuIIX(N,N)}{H+}{(N,N)XRuII(p-cym)}][PF6] (N,N = functionalised
quinaldamide and X = Cl or Br). These complexes are formed by a reaction of [p-cymRu(μ-X)2]2 with a
functionalised quinaldamide ligand. When filtered over NH4PF6, and under aerobic conditions the equilibrium
of NH4PF6 ⇔ NH3 + HPF6 enables incorporation of HPF6 and the stabilisation of two monomeric
ruthenium complexes by a bridging H+, which are counter-balanced by a PF6 counterion. X-ray crystallographic
analysis is presented for six new structures with O⋯O distances of 2.420(4)–2.448(15) Å, which is
significant for strong hydrogen bonds. Chemosensitivity studies against HCT116, A2780 and cisplatinresistant
A2780cis human cancer cells showed the ruthenium complexes with a bromide ancillary ligand
to be more potent than those with a chloride ligand. The 4’-fluoro compounds show a reduction in
potency for both chloride and bromide complexes against all cell lines, but an increase in selectivity
towards cancer cells compared to non-cancer ARPE-19 cells, with a selectivity index >1. Mechanistic
studies showed a clear correlation between IC50 values and induction of cell death by apoptosis

Identiferoai:union.ndltd.org:BRADFORD/oai:bradscholars.brad.ac.uk:10454/9487
Date01 July 2016
CreatorsLord, Rianne M., Allison, Simon J., Rafferty, K., Ghandhi, L., Pask, C.M., McGowan, P.C.
Source SetsBradford Scholars
LanguageEnglish
Detected LanguageEnglish
TypeArticle, Accepted manuscript
Rights© 2016 RSC. Reproduced with permission from the publisher in accordance with the publisher's self-archiving policy., Unspecified

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