Ruthenium(II) nitrofurylsemicarbazone complexes:: new DNA binding agents

被引:29
作者
Cabrera, E
Cerecetto, H
González, M
Gambino, D
Noblia, P
Otero, L
Parajón-Costa, B
Anzellotti, A
Sánchez-Delgado, R
Azqueta, A
de Ceráin, AL
Monge, A
机构
[1] Univ Republica, Fac Ciencias, Fac Quim, Dept Quim Organ, Montevideo 11400, Uruguay
[2] Univ Republica, Fac Quim, DEC, Catedra Quim Inorgan, Montevideo 11200, Uruguay
[3] Univ Navarra, CIFA, Unidad I&D Medicamentos, E-31080 Pamplona, Spain
[4] Inst Venezolano Invest Cient, Ctr Quim, Caracas, Venezuela
[5] Univ Nacl La Plata, Fac Ciencias Exactas, CEQUINOR, La Plata, Buenos Aires, Argentina
关键词
ruthenium complexes; DNA binding evaluations; anti-tumor activity; nitrofurylsemicarbazone;
D O I
10.1016/j.ejmech.2004.01.002
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Complexes of the type [Ru(II)Cl-2(DMSO)(2)L], where L are 5-nitrofurylsemicarbazone derivatives, were prepared in an effort to combine the potential anti-tumor activity of the metal and the free ligands. The new complexes are excellent DNA bindin agents for calf thymus DNA. So, their in vitro anti-tumor activity was tested in cellular models and the complexes were found to be non-cytotoxic on the tumor cell lines assayed neither in aerobic conditions nor in the bio-reductive assay performed. Redox behavior, lipophilicity and stability were studied in order to explain the lack of cellular cytotoxic effects. The complexes resulted 10-100 times more hydrophilic than the parent ligands thus the bio-activity of these compounds would be compromised by their inadequate lipophilic properties. (C) 2004 Elsevier SAS. All rights reserved.
引用
收藏
页码:377 / 382
页数:6
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