钌-氮杂环卡宾配合物对C6和HeLa癌细胞的抗增殖活性的合成与研究。
Synthesis and investigation of antiproliferative activity of Ru-NHC complexes against C6 and HeLa cancer cells.
作者信息
Paşahan Ramazan, Akkoç Mitat, Yaşar Şeyma, Kul Köprülü Tuğba, Tekin Şaban, Yaşar Sedat, Özdemir İsmail
机构信息
Department of Neurosurgery,, Faculty of Medicine, İnönü University, Malatya, Turkey.
Department of Property Protection and Security, Hekimhan Vocational College, Malatya Turgut Özal University, Malatya, Turkey.
出版信息
Turk J Chem. 2022 Mar 15;46(4):1097-1109. doi: 10.55730/1300-0527.3418. eCollection 2022.
The 2-methylpyridine, 2-diethylaminoethyl, and isopentyl linked a series of symmetric and unsymmetric benzimidazolium salts 2a-e were prepared and used in the synthesis of silver-N-heterocyclic carbene (NHC) complexes (3a-e). The Ru(II)-NHC complexes (4a-h) were synthesized via transmetalation reaction from 3a-e. 4a-h complexes were converted to Ru(II)-NHC.HCl complexes (5ah) by HCl solution of diethyl ether and characterized by different spectroscopic techniques such as H and C NMR, LC/MS-Q-TOF, FT-IR, elemental analysis, and melting point detection. We examined the effect of the structural difference of complexes on anticancer activity via different arenes and metal centers. Antiproliferative activity of 5a-h and 3a was tested against human cervix adenocarcinoma (HeLa) and rat glioblastoma (C6) cell lines by ELISA assay. The IC value of 5b, 5c and 5e complexes exhibited good cytotoxic activity than cisplatin on C6 (14.2 ± 0.5 mM; 16.2 ± 0.4 mM; 24.2 ± 0.7 mM, respectively) and HeLa (11.1 ± 0.5 mM; 13.7 ± 0.3 mM; 22.8 ± 0.8 mM, respectively) cell lines.
制备了一系列由2-甲基吡啶、2-二乙氨基乙基和异戊基连接的对称和不对称苯并咪唑鎓盐2a - e，并将其用于合成银-N-杂环卡宾（NHC）配合物（3a - e）。通过3a - e的金属转移反应合成了Ru(II)-NHC配合物（4a - h）。4a - h配合物通过在乙醚的HCl溶液中反应转化为Ru(II)-NHC·HCl配合物（5a - h），并通过不同的光谱技术进行表征，如氢谱和碳谱、液相色谱/质谱-四极杆飞行时间质谱、傅里叶变换红外光谱、元素分析和熔点检测。我们通过不同的芳烃和金属中心研究了配合物结构差异对抗癌活性的影响。通过酶联免疫吸附测定法测试了5a - h和3a对人宫颈腺癌（HeLa）和大鼠胶质母细胞瘤（C6）细胞系的抗增殖活性。5b、5c和5e配合物对C6细胞系（分别为14.2±0.5 mM；16.2±0.4 mM；24.2±0.7 mM）和HeLa细胞系（分别为11.1±0.5 mM；13.7±0.3 mM；22.8±0.8 mM）的IC值显示出比顺铂更好的细胞毒性活性。
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