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New Ruthenium(II)-Letrozole Complexes as Anticancer Therapeutics.

Summary of "New Ruthenium(II)-Letrozole Complexes as Anticancer Therapeutics."

Novel ruthenium-letrozole complexes have been prepared, and cell viability of two human cancer cell types (breast and glioblastoma) was determined. Some ruthenium compounds are known for their cytotoxicity to cancer cells, whereas letrozole is an aromatase inhibitor administered after surgery to post-menopausal women with hormonally responsive breast cancer. A significant in vitro activity was established for complex 5·Let against breast cancer MCF-7 cells and significantly lower activity against glioblastoma U251N cells. The activity of 5·Let was even higher than that of 4, a compound analogous to the well-known drug RAPTA-C. Results from the combination of 5·Let (or 4) with 3-methyladenine (3-MA) or with curcumin, respectively, revealed that the resultant cancer cell death likely involves 5·Let-induced autophagy.

Affiliation

Department of Pharmacology and Therapeutics, McGill University , 3655 Promenade Sir-William-Osler, Montreal, Quebec H3G 1Y6, Canada.

Journal Details

This article was published in the following journal.

Name: Journal of medicinal chemistry
ISSN: 1520-4804
Pages: 8799-806

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Medical and Biotech [MESH] Definitions

Unstable isotopes of ruthenium that decay or disintegrate emitting radiation. Ru atoms with atomic weights 93-95, 97, 103, and 105-108 are radioactive ruthenium isotopes.

Inorganic compounds that contain ruthenium as an integral part of the molecule.

An inorganic dye used in microscopy for differential staining and as a diagnostic reagent. In research this compound is used to study changes in cytoplasmic concentrations of calcium. Ruthenium red inhibits calcium transport through membrane channels.

Complexes containing CHLOROPHYLL and other photosensitive molecules. They serve to capture energy in the form of PHOTONS are generally found as components of the PHOTOSYSTEM I PROTEIN COMPLEX or the PHOTOSYSTEM II PROTEIN COMPLEX.

A hard, brittle, grayish-white rare earth metal with an atomic symbol Ru, atomic number 44, and atomic weight 101.07. It is used as a catalyst and hardener for PLATINUM and PALLADIUM.

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