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某些单核钌(II)配合物的合成与抗癌活性

Synthesis and anticancer activity of certain mononuclear Ru (II) complexes.

作者信息

Rathinasamy Suresh, Karki Subhas Somalingappa, Bhattacharya Shiladitya, Manikandan Lakshmanan, Prabakaran Senthilkumar G, Gupta Malaya, Mazumder Upal Kanti

机构信息

Division of Pharmaceutical Chemistry, Department of Pharmaceutical Technology, Jadavpur University, Kolkata 700032, India.

出版信息

J Enzyme Inhib Med Chem. 2006 Oct;21(5):501-7. doi: 10.1080/14756360600703396.

Abstract

Bis(1,10-phenanthroline/2,2'-bipyridine) ruthenium(II)complexes containing TCP, TTZ OPBI, and BTSC ligands (where, TCP = 1-thiocarbamoyl-3,5-diphenyl-2-pyrazoline, TTZ = 2-(3,5-diphenyl-4,5-dihydropyrazol-1-yl)-4-phenylthiazole, OPBI = 2-hydroxyphenyl benzimidazole and BTSC = benzoin thiosemicarbazone) have been prepared and characterized. The spectral data suggested that the ligands were coordinated with the metal through nitrogen, sulfur and oxygen atoms. The target complexes were tested in vivo for anticancer activity against transplantable murine tumor cell line, Ehrlich's Ascitic Carcinoma (EAC). All these complexes increased the life span of the EAC-bearing mice, decreased their tumor volume and viable ascitic cell count as well as improved Hb, RBC and WBC counts. These results suggest that the Ru(II) complexes exhibit significant antitumor activity in EAC-bearing mice. It was also observed that the ruthenium complexes protected red blood cells from 2,2'-azo-bis(2-methylpropionamidine) dihydrochloride (AAPH)- induced hemolysis. The inhibitory effect was dose-dependent at a concentration of 20-120 microg/ml.

摘要

已制备并表征了含有TCP、TTZ、OPBI和BTSC配体的双(1,10-菲咯啉/2,2'-联吡啶)钌(II)配合物(其中,TCP = 1-硫代甲酰基-3,5-二苯基-2-吡唑啉,TTZ = 2-(3,5-二苯基-4,5-二氢吡唑-1-基)-4-苯基噻唑,OPBI = 2-羟基苯基苯并咪唑,BTSC = 安息香硫代半卡巴腙)。光谱数据表明,配体通过氮、硫和氧原子与金属配位。对目标配合物进行了体内试验,以检测其对可移植小鼠肿瘤细胞系艾氏腹水癌(EAC)的抗癌活性。所有这些配合物均延长了荷EAC小鼠的寿命,减小了其肿瘤体积和活腹水细胞计数,并改善了血红蛋白、红细胞和白细胞计数。这些结果表明,Ru(II)配合物在荷EAC小鼠中表现出显著的抗肿瘤活性。还观察到,钌配合物可保护红细胞免受2,2'-偶氮双(2-甲基丙脒)二盐酸盐(AAPH)诱导的溶血。在20-120μg/ml的浓度下,抑制作用呈剂量依赖性。

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