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) <i>N</i>-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 <b>BGC4</b> bearing a 4-CF<sub>3</sub>-pyridyl substituent and a chloride ligand showed promising antineoplastic activity on the triple negative breast cancer cell line. <b>BGC4</b> was able to induce cell apoptosis but had no effect on the cell cycle. In vivo, <b>BGC4</b> reduced the tumor growth rate by increasing the necrosis area and decreasing the mitotic activity. Repeated injections of <b>BGC4</b> did not induce common side effects. The present investigation shows that <b>BGC4</b> 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.
Authors
- Patricia Forgez (ORCID: https://orcid.org/0000-0002-7045-0520)
- Benoı̂t Bertrand (ORCID: https://orcid.org/0000-0003-0542-4454)
- Benoît Caron (ORCID: https://orcid.org/0000-0001-7051-4339)
- Edwyn Remadna
- Jérémy Forté (ORCID: https://orcid.org/0000-0002-9363-4162)
- Julie Noël (ORCID: https://orcid.org/0000-0002-9937-885X)
- Nicolas Städler (ORCID: https://orcid.org/0000-0001-8212-7459)
- Serge Thorimbert (ORCID: https://orcid.org/0000-0002-0290-2820)
- Ingo Ott (ORCID: https://orcid.org/0000-0002-8087-4618)
- Nadia Hoyeau
- Anna Wilsmann
Institutions
- Centre National de la Recherche Scientifique (FR)
- Inserm (FR)
- Université Paris Cité (FR)
- Sorbonne Université (FR)
- Institut des Sciences de la Terre de Paris (FR)
- Assistance Publique – Hôpitaux de Paris (FR)
- Hôpital Saint-Antoine (FR)
- Institut Parisien de Chimie Moléculaire (FR)
- Observatoire des sciences de l'Univers Paris-Centre Ecce Terra
- Technische Universität Braunschweig (DE)
Publication Details
- Journal
- Journal of Medicinal Chemistry
- Published
- 2025-01-10
- DOI
- https://doi.org/10.1021/acs.jmedchem.4c02470
- Citations
- 3
- Primary Topic
- N-Heterocyclic Carbenes in Organic and Inorganic Chemistry
- Type
- article
- Field-Weighted Citation Impact
- 2.81
Funders
- Institut National de la Santé et de la Recherche Médicale
- Ministère de l'Education Nationale, de l'Enseignement Superieur et de la Recherche
- Centre National de la Recherche Scientifique
- Sorbonne Université