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- W3014580059 abstract "Sixcomplexes of formula [Ir(η5:κ1-C5Me4CH2py)(C,N)]PF6, whereC5Me4CH2py is 2-((2,3,4,5-tetramethylcyclopentadienyl)methyl)pyridine,and C,N is 2-phenylpyridine (1), 7,8-benzoquinoline (2), 1-phenylisoquinoline (3), 2-(p-tolyl)pyridine (4), 4-chloro-2-phenylquinoline (5), or 2-(2,4-difluorophenyl)pyridine (6), havebeen synthesized. The cyclopentadienyl ligand bears a tethered pyridinethat binds to the metal center, resulting in an Ir(η5:κ1-C5Me4CH2pyN) tether-ring structure, as confirmedby the X-ray crystal structures of 1, 2, 4, 5, and 6. Nontether versionsof 1 and 2 were synthesized to aid unambiguouscorrelation between structure and activity. While nontether complexesare highly potent toward MCF7 cancer cells (similar to cisplatin),complexes bearing the tether-ring structure, 1–6, are exceptionally more potent (1–2 orders of magnitude).Additionally, 1–6 disrupt mitochondrialmembrane potential (ΔΨm) andinduce oxidative stress. Internalization studies strongly correlateintracellular accumulation and anticancer activity in tether and nontethercomplexes. We present a new class of organo-iridium drug candidatesbearing a structural feature that results in a leap in anticancerpotency." @default.
- W3014580059 created "2020-04-10" @default.
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- W3014580059 date "2020-03-24" @default.
- W3014580059 modified "2023-09-23" @default.
- W3014580059 title "Structurally StrainedHalf-Sandwich Iridium(III) ComplexesAs Highly Potent Anticancer Agents" @default.
- W3014580059 doi "https://doi.org/10.1021/acs.jmedchem.9b02000.s001" @default.
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