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一些单核钌(II)配合物的合成、抗肿瘤和细胞毒性活性。

Synthesis, antineoplastic and cytotoxic activities of some mononuclear Ru(II) complexes.

机构信息

Department of Pharmaceutical Chemistry, S.R. College of Pharmacy, Ananthasagar, Warangal, Andhra Pradesh, India.

出版信息

J Enzyme Inhib Med Chem. 2010 Aug;25(4):513-9. doi: 10.3109/14756360903357577.

DOI:10.3109/14756360903357577
PMID:20128638
Abstract

A series of mononuclear Ru(II) complexes of the type Ru(S)(2)(K), where S = 1,10-phenanthroline/2,2'-bipyridine and K = 4-OH-btsz, 4-CH(3)-btsz, 3,4-di-OCH(3)-btsz, 4-OH-binh, 4-CH(3)-binh, 3,4-di-OCH(3)-binh, were prepared and characterized by elemental analysis, FTIR, (1)H-NMR, and mass spectroscopy. The complexes displayed metal-ligand charge transfer (MLCT) transitions in the visible region. These ligands formed bidentate octahedral ruthenium complexes. The title complexes were evaluated for their in vivo anticancer activity against a transplantable murine tumor cell line, Ehrlisch's ascites carcinoma (EAC), and in vitro cytotoxic activity against human cancer cell lines Molt 4/C(8) and CEM and murine tumor cell line L1210. The ruthenium complexes showed promising biological activity especially in decreasing tumor volume and viable ascites cell counts. Treatment with 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 0.21 to 24 muM against Molt 4/C(8), 0.16 to 19 microM against CEM, and 0.75 to 32 microM against L1210.

摘要

一系列单核钌(II)配合物的类型[Ru(S)(2)(K)](2+),其中 S = 1,10-菲咯啉/2,2'-联吡啶和 K = 4-OH-btsz,4-CH(3)-btsz,3,4-二-OCH(3)-btsz,4-OH-binh,4-CH(3)-binh,3,4-二-OCH(3)-binh,被制备和通过元素分析,FTIR,(1)H-NMR 和质谱法进行表征。这些配合物在可见区域显示金属-配体电荷转移(MLCT)跃迁。这些配体形成二齿八面体钌配合物。这些标题配合物被评估其对移植性小鼠肿瘤细胞系 Ehrlisch's 腹水癌(EAC)的体内抗癌活性,以及对人癌细胞系 Molt 4/C(8)和 CEM 和小鼠肿瘤细胞系 L1210 的体外细胞毒性活性。钌配合物表现出有希望的生物活性,特别是在降低肿瘤体积和活腹水细胞计数方面。用这些配合物治疗携带 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对 Molt 4/C(8)的细胞毒性活性从 0.21 到 24 μM,对 CEM 的 0.16 到 19 μM,对 L1210 的 0.75 到 32 μM。

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