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Synthesis, spectroscopic characterization, antineoplastic, in vitro-cytotoxic, and antibacterial activities of mononuclear ruthenium(II) complexes

机译:单核钌(II)配合物的合成,光谱表征,抗肿瘤,体外细胞毒性和抗菌活性

摘要

The synthesis, antineoplastic, cytotoxic, and antibacterial activities of Ru(II) complexes derived from quinazoline and thiosemicarbazone ligands are reported. These complexes have been prepared and characterized by UV-Vis, IR, H-1-NMR, FAB-mass spectroscopy, and elemental analysis. The ligands and resulting complexes were subjected to in vivo antineoplastic activity against a transplantable murine tumor cell line Ehrlich ascites carcinoma (EAC) and in vitro cytotoxic activity against human cancer cell line Molt 4/C-8, CEM, and murine tumor cell line L 1210. The ruthenium complexes show promising biological activity especially in decreasing tumor volume and viable ascitic cell counts. These complexes prolonged the life span of mice bearing EAC tumors by 10-52%. In vitro evaluation of these ruthenium complexes revealed cytotoxic activity from 0.29 to 2.9 mu mol L-1 against Molt 4/C-8, 0.22 to 2.1 mu mol L-1 against CEM and 0.42 to 4.7 mu mol L-1 against L1210 cell proliferation, depending on the nature of the compound. The metal complexes are more active than the parent ligand and exhibit mild to moderate antibacterial activity.
机译:报道了衍生自喹唑啉和硫代半脲配体的Ru(II)配合物的合成,抗肿瘤,细胞毒性和抗菌活性。这些配合物已通过紫外-可见,红外,H-1-NMR,FAB-质谱和元素分析制备并表征。使配体和所得复合物对可移植的鼠肿瘤细胞系艾氏腹水癌(EAC)进行体内抗肿瘤活性,并对人癌细胞Molt 4 / C-8,CEM和鼠肿瘤细胞系L进行体外细胞毒活性1210.钌配合物显示出有希望的生物学活性,特别是在减少肿瘤体积和存活的腹水细胞计数方面。这些复合物将带有EAC肿瘤的小鼠的寿命延长了10-52%。这些钌配合物的体外评估显示,其对Molt 4 / C-8的细胞毒活性为0.29至2.9μmolL-1,对CEM为0.22至2.1μmolL-1,对L1210细胞增殖为0.42至4.7μmolL-1。 ,取决于化合物的性质。金属络合物比母体配体更具活性,并表现出中等至中等的抗菌活性。

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