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PMID: 6283334 Published · ppublish English Journal Article Research Support, Non-U.S. Gov't Review

Nonintercalative DNA-binding antitumour compounds.

Molecular and cellular biochemistry ·Vol. 43 ·No. 3 ·1982-04-02 ·Pages 167-81

Baguley BC

Abstract

A family of compounds which appear to bind reversibly to double stranded DNA without intercalation between DNA base pairs has been defined. Methods are described by which this non-intercalative binding can be characterised using ultraviolet spectrometry, fluorimetry with ethidium as a probe, viscometry and other hydrodynamic techniques, circular dichroism and nuclear magnetic resonance spectrometry. Antibiotics which fall into this family include the antibiotics distamycin A, netropsin, mithramycin, chromomycin and olivomycin. Synthetic antitumour agents include diarylamidines such as berenil, phthalanilides, aromatic bisguanylhydrazones and bisquaternary ammonium heterocycles. A survey has been made of the general requirements of this family of compounds for DNA binding and biological activity. Binding of drugs to the minor groove of the DNA double helix appears to be the most likely mechanism for the antitumour action of these compounds.

MeSH Terms
Amidines/metabolism Anilides/metabolism Animals Antineoplastic Agents/metabolism,pharmacology Base Sequence Binding Sites Chemical Phenomena Chemistry Circular Dichroism DNA/metabolism Distamycins/metabolism Ethidium/metabolism Forecasting Guanidines/metabolism Hydrazones/metabolism Intercalating Agents/metabolism Magnetic Resonance Spectroscopy Netropsin/metabolism Nucleic Acid Conformation Plicamycin/metabolism Spectrophotometry, Ultraviolet Structure-Activity Relationship
Chemicals
Amidines Anilides Antineoplastic Agents Distamycins Guanidines Hydrazones Intercalating Agents Netropsin DNA Ethidium Plicamycin
Authors & Affiliations
1 authors, click to expand affiliations / ORCID
Baguley B C
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Article Info
Journal
Molecular and cellular biochemistry
Abbr.
Mol Cell Biochem
ISSN
0300-8177
DOI
10.1007/BF00223008
Published
1982-04-02
Pages
167-81
Language
English
Region
Netherlands
NLM ID
0364456
Subset
IM
External Links
PubMed source DOI: 10.1007/BF00223008 View journal details
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