New carbocyclic analogues of netropsin: synthesis and inhibition of topoisomerases.
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.
Department of Organic Chemistry, Medical Academy of Bialystok, Poland.
Anna
A
Pućkowska
Krzysztof
K
Bielawski
Anna
A
Bielawska
Andrzej
A
Rózański
D000970:Antineoplastic Agents / Q000378:metabolism; D004247:DNA / Q000378:metabolism; D026942:DNA Topoisomerases / Q000096:biosynthesis*; D009429:Netropsin / Q000031:analogs & derivatives*; D059003:Topoisomerase Inhibitors
D000970:Antineoplastic Agents; D059003:Topoisomerase Inhibitors; D009429:Netropsin; D004247:DNA; D026942:DNA Topoisomerases