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.
Highlights
c-Myb attenuates NF-κB activity in breast cancer.
Interaction with co-activator p300 is required for NF-κB suppression by c-Myb.
c-Myb negatively regulates IL1a transcription in several ER- breast cancer cell lines.
Inhibition of IL1α expression mediates the anti-inflammatory effect of c-Myb.
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