Synthesis and Biological Evaluation of a New Biphenyl-Based Organogold(III) Complex with In Vitro and In Vivo Anticancer Activity

Despite recent advances in cancer treatment, there is still a need
for novel compounds with antineoplastic activity. Among 11 biphenyl-based
organogold(III) N-heterocyclic carbene (NHC) (BGC)
complexes of general formula [(C^C)Au(NHC-pyr)X], where (C^C) = 4,4′-ditertbutylbiphenyl,
X = Cl or phenylacetylide, and (NHC-pyr) is a pyridyl-substituted
NHC ligand, the complex BGC4 bearing a 4-CF3-pyridyl substituent and a chloride ligand showed promising antineoplastic
activity on the triple negative breast cancer cell line. BGC4 was able to induce cell apoptosis but had no effect on the cell
cycle. In vivo, BGC4 reduced the tumor growth rate by
increasing the necrosis area and decreasing the mitotic activity.
Repeated injections of BGC4 did not induce common side
effects. The present investigation shows that BGC4 is
a promising antineoplastic candidate. Its potential as a future chemotherapy
for the treatment of cancer will be strengthened by evaluating its
efficacy in combined treatment with current chemotherapy.