SYNTHESIS, MUTAGENICITY, BINDING TO PBR-322 DNA AND ANTITUMOR-ACTIVITY OF PLATINUM(II) COMPLEXES WITH ETHAMBUTOL

被引：0

作者：

COLUCCIA, M ^{[1
]}

FANIZZI, FP ^{[1
]}

GIANNINI, G ^{[1
]}

GIORDANO, D ^{[1
]}

INTINI, FP ^{[1
]}

LACIDOGNA, G ^{[1
]}

LOSETO, F ^{[1
]}

MARIGGIO, MA ^{[1
]}

NASSI, A ^{[1
]}

NATILE, G ^{[1
]}

机构：

[1] DIPARTIMENTO FARM CHIM,I-70126 BARI,ITALY

来源：

ANTICANCER RESEARCH | 1991年 / 11卷 / 01期

关键词：

ENANTIOMERIC PLATINUM COMPLEXES; DNA-BINDING; MUTAGENICITY; ANTITUMOR ACTIVITY;

D O I：

暂无

中图分类号：

R73 [肿瘤学];

学科分类号：

100214 ;

摘要：

Platinum complexes with N,N'-bis(1-hydroxybut-2yl)ethylenediamine, [PtCl2(ethambutol)] were prepared and the biological activity of three isomers [with (-), (+) and (+/-) ethambutol, respectively] investigated. All species interact with the Bam HI and Ava I recognition sequences showing a binding preference for GC rich sequences of DNA. The complex which showed the greatest interaction with adjacent guanines, [PtCl2{(+/-)ethambutol}] was also found to be the most mutagenic of the three. On the other hand, only [PtCl2{(+)ethambutol}] had a considerable antitumour activity against both P388 leukaemia and Lewis lung carcinoma, and this was not correlated either with restriction enzyme blocking activity or with mutagenicity.

引用

页码：281 / 287

页数：7

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