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Ruthenium(II)-Tris-pyrazolylmethane Complexes Inhibit Cancer Cell Growth by Disrupting Mitochondrial Calcium Homeostasis

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ČERVINKA Jakub GOBBO Alberto BIANCALANA Lorenzo MARKOVÁ Lenka NOVOHRADSKÝ Vojtěch GUELFI Massimo ZACCHINI Stefano KAŠPÁRKOVÁ Jana BRABEC Viktor MARCHETTI Fabio

Rok publikování 2022
Druh Článek v odborném periodiku
Časopis / Zdroj Journal of Medicinal Chemistry
Fakulta / Pracoviště MU

Přírodovědecká fakulta

Citace
www https://pubs.acs.org/doi/10.1021/acs.jmedchem.2c00722
Doi http://dx.doi.org/10.1021/acs.jmedchem.2c00722
Klíčová slova Metallodrugs; Ruthenium; Anticancer activity; Cell death; Calcium homeostasis
Přiložené soubory
Popis While ruthenium arene complexes have been widely investigated for their medicinal potential, studies on homologous compounds containing a tridentate tris(1-pyrazolyl)methane ligand are almost absent in the literature. Ruthenium(II) complex 1 was obtained by a modified reported procedure; then, the reactions with a series of organic molecules (L) in boiling alcohol afforded novel complexes 2-9 in 77-99% yields. Products 2-9 were fully structurally characterized. They are appreciably soluble in water, where they undergo partial chloride/water exchange. The antiproliferative activity was determined using a panel of human cancer cell lines and a noncancerous one, evidencing promising potency of 1, 7, and 8 and significant selectivity toward cancer cells. The tested compounds effectively accumulate in cancer cells, and mitochondria represent a significant target of biological action. Most notably, data provide convincing evidence that the mechanism of biological action is mediated by the inhibiting of mitochondrial calcium intake.

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