INTERCALATIVE BINDING TO DNA OF ANTI-TUMOR DRUGS DERIVED FROM 3-NITRO-1,8-NAPHTHALIC ACID

被引：88

作者：

WARING, MJ ^{[1
]}

GONZALEZ, A ^{[1
]}

JIMENEZ, A ^{[1
]}

VAZQUEZ, D ^{[1
]}

机构：

[1] MED SCH,DEPT PHARMACOL,CAMBRIDGE CB2 2QD,ENGLAND

来源：

NUCLEIC ACIDS RESEARCH | 1979年 / 7卷 / 01期

基金：

英国医学研究理事会;

关键词：

D O I：

10.1093/nar/7.1.217

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：

Two new antitumour drugs, imide derivatives of 3-nitro-1, 8-naphthalic acid having different basic side chains linked to the imide nitrogen, have been shown to bind to double-helical DNA by intercalation. At ionic strength 0.01 mol/litre, pH 7, their intrinsic association constants are about 1.45 × 105 M-1 and each bound ligand molecule occludes about 3.4 nucleotides of the DNA lattice. They remove and reverse the supercoiling of closed circular duplex PM2 DNA with apparent unwinding angles of 11-12° per bound drug molecule, referred to an assumed unwinding angle of 26° for ethidium. They increase the viscosity of sonicated rod-like DNA fragments, each bound drug molecule producing a calculated increment in length of 2.2 - 2.5 Å. No important differences between the DNA-binding characteristics of the two drugs were detected, though one appears marginally more active than the other in certain biological tests. © 1979 Information Retrieval Limited.

引用

页码：217 / 230

页数：14

共 36 条

[1] INTERACTION OF PHENOSAFRANINE WITH NUCLEIC-ACIDS AND MODEL POLYPHOSPHATES .2. CHARACTERIZATION OF PHENOSAFRANINE BINDING TO DNA [J].