Photochemistry and anticancer activity of Pt(IV)Re(I) conjugates.

The photophysical and photochemical properties of two Pt(IV)Re(I) conjugates were studied both experimental and computational methods. Both conjugates exhibit modest photocytotoxicity against ovarian cancer cells. X-ray fluorescence microscopy showed that Pt and Re colocalize in cells whether they had been irradiated or not.

Triazolyl-Functionalized N-Heterocyclic Carbene Half-Sandwich Compounds: Coordination Mode, Reactivity and in vitro Anticancer Activity.

We report investigations on the anticancer activity of organometallic [M (η -p-cymene/η -pentamethylcyclopentadienyl)] (M=Ru, Os, Rh, and Ir) complexes of N-heterocyclic carbenes (NHCs) substituted with a triazolyl moiety. Depending on the precursors, the NHC ligands displayed either mono- or bidentate coordination via the NHC carbon atom or as N,C-donors. The metal complexes were investigated for their stability in aqueous solution, with the interpretation supported by density functional theory calculations, and reactivity to biomolecules.

Application of X-ray absorption and X-ray fluorescence techniques to the study of metallodrug action.

X-ray absorption spectroscopy and X-ray fluorescence microscopy are two synchrotron-based techniques frequently deployed either individually or in tandem to investigate the fates of metallodrugs and their biotransformation products in physiologically relevant sample material. These X-ray methods confer advantages over other analytical techniques in that they are nondestructive and require minimal chemical or physical manipulation of the sample before analysis, conserving both chemical and spatial information of the element(s) under investigation. In this review, we present selected examples of the use of X-ray absorption spectroscopy and X-ray fluorescence microscopy in studies of metallodrug speciation and localisation in vivo, in cell spheroids and in intact tissues and organs, and offer recent highlights in the advances of these techniques as they pertain to research on metallodrug action.

Thiourea-Derived Chelating Ligands and Their Organometallic Compounds: Investigations into Their Anticancer Activity.

Thiones have been investigated as ligands in metal complexes with catalytic and biological activity. We report the synthesis, characterization, and biological evaluation of a series of M complexes of the general formulae [M(cym)(L)Cl]X (cym = η--cymene) or [M(Cp*)(L)Cl]X (Cp* = η-pentamethylcyclopentadienyl), where X = Cl or PF, and L represents heterocyclic derivatives of thiourea. The thiones feature a benzyl-triazolyl pendant and they act as bidentate ligands via ,-coordination to the metal centers.

X-Ray fluorescence microscopy reveals that rhenium(i) tricarbonyl isonitrile complexes remain intact in vitro.

The complex fac-[Re(CO)3(dmphen)(para-tolylisonitrile)]+ (TRIP), where dmphen = 2,9-dimethyl-1,10-phenanthroline, is an endoplasmic reticulum stress-inducing anticancer agent (A. P. King, S.

Potent Inhibition of Thioredoxin Reductase by the Rh Derivatives of Anticancer M(arene/Cp*)(NHC)Cl Complexes.

Metal complexes provide a versatile platform to develop novel anticancer pharmacophores, and they form stable compounds with -heterocyclic carbene (NHC) ligands, some of which have been shown to inhibit the cancer-related selenoenzyme thioredoxin reductase (TrxR). To expand a library of isostructural NHC complexes, we report here the preparation of Rh- and Ir(Cp*)(NHC)Cl (Cp* = η-pentamethylcyclopentadienyl) compounds and comparison of their properties to the Ru- and Os(cym) analogues (cym = η--cymene). Like the Ru- and Os(cym) complexes, the Rh- and Ir(Cp*) derivatives exhibit cytotoxic activity with half maximal inhibitory concentration (IC) values in the low micromolar range against a set of four human cancer cell lines.

Redox Stability Controls the Cellular Uptake and Activity of Ruthenium-Based Inhibitors of the Mitochondrial Calcium Uniporter (MCU).

The mitochondrial calcium uniporter (MCU) is the ion channel that mediates Ca uptake in mitochondria. Inhibitors of the MCU are valuable as potential therapeutic agents and tools to study mitochondrial Ca . The best-known inhibitor of the MCU is the ruthenium compound Ru360.

Confocal Volumetric μXRF and Fluorescence Computed μ-Tomography Reveals Arsenic Three-Dimensional Distribution within Intact Fronds.

The fern has been the subject of numerous studies because of its extreme arsenic hyperaccumulation characteristics. However, information on the arsenic chemical speciation and distribution across cell types within intact frozen-hydrated fronds is necessary to better understand the arsenic biotransformation pathways in this unusual fern. While 2D X-ray absorption spectroscopy imaging studies show that different chemical forms of arsenic, As(III) and As(V), occur across the plant organs, depth-resolved information on arsenic distribution and chemical speciation in different cell types within tissues of have not been reported.