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

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

  • J Med Chem. 2025 Jan 23;68(2):1755-1771. doi: 10.1021/acs.jmedchem.4c02470.
Edwyn Remadna 1 2,  Anna Wilsmann 3,  Nicolas Stadler 2,  Jérémy Forté 1,  Nadia Hoyeau 4,  Ingo Ott 3,  Julie Noël 5,  Benoît Caron 6,  Serge Thorimbert 1,  Patricia Forgez 2,  Benoît Bertrand 1
Affiliations

Affiliations

  • 1 Sorbonne Université, CNRS Institut Parisien de Chimie Moléculaire, IPCM, F-75005 Paris, France.
  • 2 Université Paris Cité, INSERM, Health & Functional Exposomics - HealthFex, U1124, Saint Germain des Prés Campus, 75006, Paris, France.
  • 3 Institute of Medicinal and Pharmaceutical Chemistry, Technische Universität Braunschweig, 38106 Braunschweig, Germany.
  • 4 Department of Pathology, Saint-Antoine Hospital, AP-HP, Sorbonne Université, 75012 Paris, France.
  • 5 Sorbonne Université, OSU Ecce Terra, F-75005 Paris, France.
  • 6 Institut des Sciences de la Terre de Paris (ISTeP), Sorbonne Université, CNRS-INSU, F-75005 Paris, France.
PMID: 39792795 DOI: 10.1021/acs.jmedchem.4c02470
Abstract

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.

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