Allison Matthew, Caramés-Méndez Pablo, Hofmann Benjamin J, Pask Christopher M, Phillips Roger M, Lord Rianne M, McGowan Patrick C
School of Chemistry, University of Leeds, Woodhouse Lane, Leeds LS2 9JT, U.K.
Department of Pharmacy, University of Huddersfield, Huddersfield HD1 3DH, U.K.
Organometallics. 2023 Jul 5;42(15):1869-1881. doi: 10.1021/acs.organomet.2c00553. eCollection 2023 Aug 14.
The synthesis and characterization of 24 ruthenium(II) arene complexes of the type [(-cym)RuCl(Fc-acac)] (where -cym = p-cymene and Fc-acac = functionalized ferrocenyl β-diketonate ligands) are reported, including single-crystal X-ray diffraction for 21 new complexes. Chemosensitivity studies have been conducted against human pancreatic carcinoma (MIA PaCa-2), human colorectal adenocarcinoma -wildtype (HCT116 ) and normal human retinal epithelial cell lines (APRE-19). The most active complex, which contains a 2-furan-substituted ligand (), is 5x more cytotoxic than the analogs 3-furan complex () against MIA PaCa-2. Several complexes were screened under hypoxic conditions and at shorter-time incubations, and their ability to damage DNA was determined by the comet assay. Compounds were also screened for their potential to inhibit the growth of both bacterial and fungal strains.
报道了24种[(-cym)RuCl(Fc-acac)]类型的钌(II)芳烃配合物（其中-cym = 对异丙基苯，Fc-acac = 功能化二茂铁基β-二酮配体）的合成与表征，包括对21种新配合物的单晶X射线衍射分析。已针对人胰腺癌（MIA PaCa-2）、人结肠直肠腺癌野生型（HCT116）和正常人视网膜上皮细胞系（APRE-19）进行了化学敏感性研究。活性最高的配合物含有2-呋喃取代配体（），对MIA PaCa-2的细胞毒性比3-呋喃类似物配合物（）高5倍。在缺氧条件下和较短孵育时间下对几种配合物进行了筛选，并通过彗星试验测定了它们损伤DNA的能力。还筛选了化合物抑制细菌和真菌菌株生长的潜力。
