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

• Authors: Anna Pućkowska , Krzysztof Bielawski , Anna Bielawska , Andrzej Róański
• Languages of publication: EN

Abstracts

EN

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 μM concentration.

Keywords

EN

topoisomerase inhibition; DNA interaction; lexitropsin; carbocyclic analogues of netropsin

• Publisher: Polish Biochemical Society
• Journal: Acta Biochimica Polonica
• Year: 2002
• Volume: 49
• Issue: 1
• Pages: 177-183

Dates

published

2002

received

2001-09-10

revised

2001-12-20

accepted

2002-01-28

Contributors

author

Anna Pućkowska

• Department of Organic Chemistry, Medical Academy of Bialystok, A. Mickiewicza 2c, 15-230 Białystok, Poland

author

Krzysztof Bielawski

• Department of Medicinal Chemistry and Drug Technology, Medical Academy of Bialystok, A. Mickiewicza 2c, 15-230 Białystok, Poland

author

Anna Bielawska

• Department of Medicinal Chemistry and Drug Technology, Medical Academy of Bialystok, A. Mickiewicza 2c, 15-230 Białystok, Poland

author

Andrzej Róański

• Department of Organic Chemistry, Medical Academy of Bialystok, A. Mickiewicza 2c, 15-230 Białystok, Poland

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