Synthesis, characterization and biological activity of trans-platinum(II) and trans-platinum(IV) complexes with 4-hydroxymethylpyridine

被引：21

作者：

Martínez, A

Lorenzo, J

Prieto, MJ

de Llorens, R

Font-Bardia, M

Solans, X

Avilés, FX

Moreno, V

机构：

[1] Univ Barcelona, Dept Quim Inorgan, E-08028 Barcelona, Spain

[2] Univ Autonoma Barcelona, Inst Biotecnol & Biomed, E-08193 Barcelona, Spain

[3] Univ Barcelona, Dept Microbiol, E-08028 Barcelona, Spain

[4] Univ Girona, Dept Biol, Girona 17071, Spain

[5] Univ Barcelona, Dept Cristallografia Mineral & Diposits Minerals, E-08028 Barcelona, Spain

来源：

CHEMBIOCHEM | 2005年 / 6卷 / 11期

关键词：

ab initio calculations; antitumor agents; apoptosis; bioinorganic chemistry; DNA; platinum;

D O I：

10.1002/cbic.200500108

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The synthesis and chemical characterisation of two new trans-platnium complexes, trans-[PtCl4NH3(4-hydroxymethylpyridine)] (1) and trans-[PtCl4NH3(4-hydroxymethylpyridine)] (2) are described. Their ability to interact with 5'-GMP by themselves and in the presence of reducing agents in the case of trans-[PTCl4NH3(4-hydroxymethylpyridine)] were tested. Circular dichroism, electrophoretic mobility in agarose gel, and atomic force microscopy studies showed that the interaction of complex 1 with DNA is stronger than that of complex 2. Cytotoxicity tests against HL-60 tumor cells also showed higher activity for trans[PtCl2NH3(4-hydroxymethylpyridine)] than for trans-[PtCl4NH3(4-hydroxymethylpyridine)]. Complex I presents similar behavior to cisplatin, but with a lower IC50 at 24 h. Complex I also showed high apoptosis induction.

引用

页码：2068 / 2077

页数：10

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