化学
体内
配体(生物化学)
细胞凋亡
联苯
体外
化疗
癌症
卡宾
药理学
取代基
立体化学
癌症研究
细胞
生物化学
受体
内科学
生物
医学
有机化学
生物技术
催化作用
作者
Edwyn Remadna,Anna Wilsmann,Nicolas Städler,Jérémy Forté,Nadia Hoyeau,Ingo Ott,Julie Noël,Benoît Caron,Serge Thorimbert,Patricia Forgez,Benoı̂t Bertrand
标识
DOI:10.1021/acs.jmedchem.4c02470
摘要
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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