化学
钌
特里斯
线粒体
钙
作用机理
癌细胞
钌红
生物活性
细胞生长
立体化学
癌症
生物化学
体外
催化作用
有机化学
医学
内科学
作者
Jakub Cervinka,Alberto Gobbo,Lorenzo Biancalana,Lenka Markova,Vojtech Novohradsky,Massimo Guelfi,Stefano Zacchini,Jana Kasparkova,Viktor Brabec,Fabio Marchetti
标识
DOI:10.1021/acs.jmedchem.2c00722
摘要
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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