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

Anna Pućkowska | Zendy; Krzysztof Bielawski | Zendy; Anna Bielawska | Zendy; Andrzej Różański | Zendy

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

Author(s) -

Anna Pućkowska,

Krzysztof Bielawski,

Anna Bielawska,

Andrzej Różański

Publication year - 2002

Publication title -

acta biochimica polonica

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.452

H-Index - 78

eISSN - 1734-154X

pISSN - 0001-527X

DOI - 10.18388/abp.2002_3834

Subject(s) - netropsin , topoisomerase , chemistry , stereochemistry , in vitro , pbr322 , plasmid , dna , biochemistry , minor groove

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.

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