A Comparative Analysis of the In Vitro Anticancer Activity of Iridium(III) {η-CMeR} Complexes with Variable R Groups.

Piano-stool iridium complexes based on the pentamethylcyclopentadienyl ligand (Cp*) have been intensively investigated as anticancer drug candidates and hold much promise in this setting. A systematic study aimed at outlining the effect of Cp* mono-derivatization on the antiproliferative activity is presented here. Thus, the dinuclear complexes [Ir(η-CMeR)Cl(μ-Cl)] (R = Me, ; R = H, ; R = Pr, ; R = 4-CHF, ; R = 4-CHOH, ), their 2-phenylpyridyl mononuclear derivatives [Ir(η-CMeR)(k,kPhPy)Cl] (), and the dimethylsulfoxide complex [Ir{η-CMe(4-CHOH)}Cl(κ-MeS=O)] () were synthesized, structurally characterized, and assessed for their cytotoxicity towards a panel of six human and rodent cancer cell lines (mouse melanoma, B16; rat glioma, C6; breast adenocarcinoma, MCF-7; colorectal carcinoma, SW620 and HCT116; ovarian carcinoma, A2780) and one primary, human fetal lung fibroblast cell line (MRC5).

Ru(ii) water oxidation catalysts with 2,3-bis(2-pyridyl)pyrazine and tris(pyrazolyl)methane ligands: assembly of photo-active and catalytically active subunits in a dinuclear structure.

Two mononuclear Ru(ii) complexes, i.e. [RuCl(κN-terpy)(κN-dpp)]PF ([1]PF; terpy = 2,2':6',2''-terpyridine; dpp = 2,3-bis(2'-pyridyl-pyrazine) and [RuCl(κN-tpm)(κN-dpp)]Cl ([2]Cl; tpm = tris(1-pyrazolyl)methane), and one dinuclear complex, i.

A biotin-conjugated photo-activated CO-releasing molecule (biotinCORM): efficient CO-release from an avidin-biotinCORM protein adduct.

Biotinylated pharmaceuticals are of great interest due to the strong interactions between biotinyl-functionality and streptavidin/avidin, which opens up avenues for efficient targeting and localisation. Three new carbon monoxide-releasing molecules (CO-RMs) have been synthesised and characterised using chemical and biological analysis. An alkyne-containing CO-RM 2 was found to be toxic to RAW 264.

A general strategy to add diversity to ruthenium arene complexes with bioactive organic compounds via a coordinated (4-hydroxyphenyl)diphenylphosphine ligand.

Esterification of (4-hydroxyphenyl)diphenylphosphine, coordinated to the [Ru(η-p-cymene)Cl] fragment, allows a series of bioactive carboxylic acids to be introduced directly into the organometallic molecule. Evaluation of the compounds on human ovarian cancer cells reveals synergistic enhancements in their antiproliferative activity relative to their bioactive organic and organometallic precursors.