Antiangiogenic Activity of Mononuclear Copper(II) Polypyridyl Complexes for the Treatment of Cancers

A series
of four new mononuclear copper­(II) polypyridyl complexes
(1–4) have been designed, developed,
and thoroughly characterized by several physicochemical techniques.
The CT-DNA binding properties of 1–4 have been investigated by absorption, emission spectroscopy, and
viscosity measurements. All the complexes especially 1 and 4 exhibit cytotoxicity toward several cancer cell
lines, suggesting their anticancer properties as observed by several
in vitro assays. Additionally, the complexes show inhibition of endothelial
cell (HUVECs) proliferation, indicating their antiangiogenic nature.
In vivo chick embryo angiogenesis assay again confirms the antiangiogenic
properties of 1 and 4. The formation of
excessive intracellular ROS (H2O2 and O2•–) and upregulation of BAX induced
by copper­(II) complexes may be the plausible mechanisms behind their
anticancer activities. The present study may offer a basis for the
development of new transition metal complexes through suitable choice
of ligands for cancer therapeutics by controlling tumor angiogenesis.