Synthesis, characterization, antitumor, and cytotoxic activity of mononuclear Ru(II) complexes

被引:9
|
作者
Thota, Sreekanth [1 ]
Karki, Subhas Somalingappa [2 ]
Jayaveera, K. N. [3 ]
Balzarini, Jan [4 ]
De Clercq, Erik [4 ]
机构
[1] SR Coll Pharm, Dept Pharmaceut Chem, Warangal 506371, Andhra Pradesh, India
[2] KLE Acad Higher Educ & Res, Coll Pharm, Dept Pharmaceut Chem, Bangalore 560010, Karnataka, India
[3] JNTU Oil Technol Res Inst, Dept Chem, Anantapur 515001, Andhra Pradesh, India
[4] Katholieke Univ Leuven, Rega Inst Med Res, B-3000 Louvain, Belgium
关键词
Ru(II) complexes; Antitumor; EAC; Cytotoxicity; MOLECULAR-STRUCTURE; CELL-GROWTH; INHIBITION; BINDING;
D O I
10.1080/00958972.2010.534140
中图分类号
O61 [无机化学];
学科分类号
070301 ; 081704 ;
摘要
In the search for antitumor active metal complexes several ruthenium complexes have been reported to be promising. A series of mononuclear Ru(II) complexes, [Ru(T)2(S)]2+, where T = 2,2'-bipyridine/1,10-phenanthroline and S = CH3-bitsz, Cl-bitsz, Br-bitsz, tmtsz, dmtsz, have been prepared and characterized by UV-Vis, IR, 1H-NMR, FAB-mass spectroscopy, and elemental analysis. The complexes were subjected to invivo anticancer activity against a transplantable murine tumor cell line Ehrlich's ascitic carcinoma (EAC) and invitro cytotoxic activity against human cancer cell line Molt 4/C8, CEM, and murine tumor cell line L1210. Ruthenium complexes showed promising biological activity especially in decreasing tumor volume and viable ascitic cell counts. Treatment with these complexes prolonged the life span of EAC-tumor-bearing mice by 10-48%. Invitro evaluation of these ruthenium complexes revealed cytotoxic activity from 0.21 to 24 mu mol L-1 against Molt 4/C8, 0.16-19 mu mol L-1 against CEM, and 0.75-32 mu mol L-1 against L1210 cell proliferation, depending on the nature of the compound.
引用
收藏
页码:4332 / 4346
页数:15
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