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

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2004年 / 39卷 / 04期

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

页码：377 / 382

页数：6

共 35 条

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