The influence of calcium ions on the DNA binding behaviour of a new platinum(II) compound linked to an amino phosphonic acid

被引:16
作者
Einhauser, TJ [1 ]
Galanski, M [1 ]
Vogel, E [1 ]
Keppler, BK [1 ]
机构
[1] UNIV HEIDELBERG,INST ANORGAN CHEM,D-69120 HEIDELBERG,GERMANY
关键词
osteotropic platinum phosphonic acid complexes; calcium ions; DNA binding behaviour; antitumour activity;
D O I
10.1016/S0020-1693(96)05477-1
中图分类号
O61 [无机化学];
学科分类号
070301 ; 081704 ;
摘要
The binding behaviour towards DNA of the new osteatropic platinum phosphonato complex [cis-Pt(NH3)(2)(sPMAA)], 1, (BPMAA = bis( phosphonomethyl) aminoacetic acid),has been investigated. The slow hydrolysis kinetics of 1 and the low antitumour activity in vitro is in contrast to the antitumour activity found in vivo. This strongly suggests an activation mechanism facilitating the formation of an adduct with DNA. The fact that a dramatic increase in the binding rate can be observed in the presence of Ca2+ ions and the fact that there is an increased calcium concentration in the region of bone tumours may explain the antitumour activity of 1 against bone tumours.
引用
收藏
页码:265 / 268
页数:4
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