Quantum mechanics

Catalysis

Cytoplasm

Biology

Photodynamic therapy

Photochemistry

Rhodium

Cancer research

Biochemistry

Melanoma

Stereochemistry

Cytotoxicity

Genetics

Physics

Organic chemistry

Porphyrin

In vitro

Fluorescence

Internal medicine

Ruthenium

Medicine

Chemistry

Fluorescence microscope

Cancer

Moiety

Cancer cell

Journal of Medicinal Chemistry

Five 5,10,15,20-tetra(4-pyridyl)porphyrin (TPP) areneruthenium(II) derivatives and a p-cymeneosmium and two pentamethylcyclopentadienyliridium and -rhodium analogues were prepared and characterized as potential photosensitizing chemotherapeutic agents. The biological effects of all these derivatives were assessed on human melanoma tumor cells, and their cellular uptake and intracellular localization were determined. All molecules, except the rhodium complex which was not cytotoxic, demonstrated comparable cytotoxicity in the absence of laser irradiation. The ruthenium complexes exhibited excellent phototoxicities toward melanoma cells when exposed to laser light at 652 nm. Cellular uptake and localization microscopy studies of [Ru 4(eta (6)-C 6H 5CH 3) 4(TPP)Cl 8] and [Rh 4(eta (5)-C 5Me 5) 4(TPP)Cl 8] revealed that they accumulated in the melanoma cell cytoplasm in granular structures different from lysosomes. The fluorescent porphyrin moiety and the metal component were localized in similar structures within the cells. Thus, the porphyrin areneruthenium(II) derivatives represent a promising new class of organometallic photosensitizers able to combine chemotherapeutic activity with photodynamic therapeutic treatment of cancer.

Ruthenium Porphyrin Compounds for Photodynamic Therapy of Cancer