Remadna Edwyn, Wilsmann Anna, Stadler Nicolas, Forté Jérémy, Hoyeau Nadia, Ott Ingo, Noël Julie, Caron Benoît, Thorimbert Serge, Forgez Patricia, Bertrand Benoît
Sorbonne Université, CNRS Institut Parisien de Chimie Moléculaire, IPCM, F-75005 Paris, France.
Université Paris Cité, INSERM, Health & Functional Exposomics - HealthFex, U1124, Saint Germain des Prés Campus, 75006, Paris, France.
J Med Chem. 2025 Jan 23;68(2):1755-1771. doi: 10.1021/acs.jmedchem.4c02470. Epub 2025 Jan 10.
Despite recent advances in cancer treatment, there is still a need for novel compounds with antineoplastic activity. Among 11 biphenyl-based organogold(III) -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 bearing a 4-CF-pyridyl substituent and a chloride ligand showed promising antineoplastic activity on the triple negative breast cancer cell line. was able to induce cell apoptosis but had no effect on the cell cycle. In vivo, reduced the tumor growth rate by increasing the necrosis area and decreasing the mitotic activity. Repeated injections of did not induce common side effects. The present investigation shows that 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.
尽管癌症治疗最近取得了进展，但仍需要具有抗肿瘤活性的新型化合物。在通式为[(C^C)Au(NHC-pyr)X]的11种基于联苯的有机金(III)-杂环卡宾(NHC)(BGC)配合物中，其中(C^C)=4,4'-二叔丁基联苯，X=Cl或苯乙炔基，且(NHC-pyr)是吡啶基取代的NHC配体，带有4-CF-吡啶基取代基和氯配体的配合物在三阴性乳腺癌细胞系上显示出有前景的抗肿瘤活性。能够诱导细胞凋亡，但对细胞周期没有影响。在体内，通过增加坏死面积和降低有丝分裂活性降低了肿瘤生长速率。重复注射没有诱导常见的副作用。目前的研究表明是一种有前景的抗肿瘤候选物。通过评估其与当前化疗联合治疗的疗效，其作为未来癌症治疗化疗药物的潜力将得到增强。
