Article Dans Une Revue Journal of Medicinal Chemistry Année : 2025

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

Benoît Bertrand

Résumé

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 (BGC) complexes of the general formula [(C^C)Au(NHC-pyr)X], where (C^C) = 4,4'-diterbutylbiphenyl, 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.

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hal-04883531 , version 1 (13-01-2025)

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Edwyn Remadna, Anna Wilsmann, Nicolas Stadler, Jérémy Forté, Nadia Hoyeau, et al.. Synthesis and Biological Evaluation of a New Biphenyl-Based Organogold(III) Complex with In Vitro and In Vivo Anticancer Activity. Journal of Medicinal Chemistry, 2025, 68 (2), pp.1755-1771. ⟨10.1021/acs.jmedchem.4c02470⟩. ⟨hal-04883531⟩
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