Department of Chemistry, Federal University of Juiz de Fora, Campus Martelos, Juiz de Fora, MG, 36036-900, Brazil.
Department of Research on Natural Products, University of Franca, Franca, SP, 14406-600, Brazil.
Biometals. 2017 Dec;30(6):841-857. doi: 10.1007/s10534-017-0046-6. Epub 2017 Aug 24.
Novel lipophilic gold(I) complexes containing 1,3,4-oxadiazol-2-thione or 1,3-thiazolidine-2-thione derivatives were synthesized and characterized by IR, high resolution mass spectrometry, and H, C P NMR. The cytotoxicity of the compounds was evaluated considering cisplatin and/or auranofin as reference in different tumor cell lines: colon cancer (CT26WT), metastatic skin melanoma (B16F10), breast adenocarcinoma (MCF-7), cervical carcinoma (HeLa), glioblastoma (M059 J). Normal human lung fibroblasts (GM07492-A) and kidney normal cell (BHK-21) were also evaluated. The gold(I) complexes were more active than their respective free ligands and cisplatin. Furthermore, antibacterial activity was evaluated against Gram-positive bacteria Staphylococcus aureus ATCC 25213, Staphylococcus epidermidis ATCC 12228 and Gram-negative bacteria Escherichia coli ATCC 11229 and Pseudomonas aeruginosa ATCC 27853 and expressed as the minimum inhibitory concentration (MIC). The complexes exhibited lower MIC values when compared to the ligands and chloramphenicol against Gram-positive bacteria and Gram-negative bacteria. Escherichia coli was sensitive one to the action of gold(I) complexes.
新型含 1,3,4-噁二唑-2-硫酮或 1,3-噻唑烷-2-硫酮衍生物的亲脂性金（I）配合物被合成并通过红外光谱、高分辨率质谱和 H、C P NMR 进行了表征。考虑到顺铂和/或金诺芬作为参考，在不同的肿瘤细胞系中评估了化合物的细胞毒性：结肠癌（CT26WT）、转移性皮肤黑色素瘤（B16F10）、乳腺腺癌（MCF-7）、宫颈癌细胞（HeLa）、神经胶质瘤（M059 J）。还评估了正常人类肺成纤维细胞（GM07492-A）和肾正常细胞（BHK-21）。金（I）配合物比其各自的游离配体和顺铂更具活性。此外，还评估了这些配合物对革兰氏阳性菌金黄色葡萄球菌 ATCC 25213、表皮葡萄球菌 ATCC 12228 和革兰氏阴性菌大肠杆菌 ATCC 11229 和铜绿假单胞菌 ATCC 27853 的抗菌活性，并以最小抑菌浓度（MIC）表示。与配体和氯霉素相比，这些配合物对革兰氏阳性菌和革兰氏阴性菌的 MIC 值更低。大肠杆菌对金（I）配合物的作用敏感。
