Synthesis and study of a new adenine-acridine tandem, inhibitor of exonuclease III

P Belmont; M Demeunynck; J F Constant; J Lhomme

doi:10.1016/s0960-894x(99)00681-2

Synthesis and study of a new adenine-acridine tandem, inhibitor of exonuclease III

Bioorg Med Chem Lett. 2000 Feb 7;10(3):293-5. doi: 10.1016/s0960-894x(99)00681-2.

Authors

P Belmont¹, M Demeunynck, J F Constant, J Lhomme

Affiliation

¹ LEDSS, Chimie Bioorganique, UMR CNRS 5616, Université Joseph Fourier, Grenoble, France.

PMID: 10698457
DOI: 10.1016/s0960-894x(99)00681-2

Abstract

A new heterodimer adenine-chain-acridine containing a mixed amido-guanidinium linker chain was synthesized. To achieve the synthesis a new method of introduction of aminoalkyl chain at position 9 of adenine was designed. The heterodimer interacts specifically with the abasic sites in DNA and inhibits the major base excision repair enzyme in Escherichia coli, Exonuclease III.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Acridines / chemistry*
Adenine / chemistry*
Animals
DNA / chemistry
DNA / drug effects
DNA Repair
Drug Screening Assays, Antitumor
Enzyme Inhibitors / chemical synthesis*
Enzyme Inhibitors / pharmacology*
Escherichia coli / enzymology
Exodeoxyribonucleases / antagonists & inhibitors*
Humans
Mice
Tumor Cells, Cultured

Substances

Acridines
Enzyme Inhibitors
DNA
Exodeoxyribonucleases
exodeoxyribonuclease III
Adenine