New carbocyclic analogues of netropsin: synthesis and inhibition of topoisomerases.

Anna Pućkowska; Krzysztof Bielawski; Anna Bielawska; Andrzej Rózański

doi:10.18388/abp.2002_3834

New carbocyclic analogues of netropsin: synthesis and inhibition of topoisomerases.

Anna Pućkowska Department of Organic Chemistry, Medical Academy of Bialystok, Poland.;
Krzysztof Bielawski
Anna Bielawska
Andrzej Rózański

DOI: https://doi.org/10.18388/abp.2002_3834

Abstract

A series of carbocyclic analogues of netropsin were synthesized and evaluated for their capacity to inhibit human topoisomerases I and II in vitro. The compounds are oligopeptides containing 1,4-di- and 1,2,5-trisubstituted benzene rings and unsubstituted N-terminal NH2 groups. Compounds 4-7 consist of two netropsin-like units linked by aliphatic (tetra- and hexamethylene) chains. In the topoisomerase I and II assay, the relaxation of pBR322 plasmid was inhibited by compounds 4-7 at 100 microM concentration.

Published

2002-03-31

Issue

Vol. 49 No. 1 (2002)

Section

Articles

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