New carbocyclic lexitropsins with dinitromustard as N-terminal fragment. Inhibition of topoisomerases.
A series of carbocyclic lexitropsins was evaluated for their capacity to inhibit human topoisomerases I and II. The synthesized compounds were carbocyclic oligopeptides with dinitromustard as N-terminal fragment. In the topoisomerases I and II assays, the relaxation of DNA were inhibited with all four compounds. This inhibition was directly proportional to the compound concentration.
D004264:DNA Topoisomerases, Type I / Q000378:metabolism; D004250:DNA Topoisomerases, Type II / Q000378:metabolism; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D009429:Netropsin / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology*; D009588:Nitrogen Mustard Compounds / Q000737:chemistry / Q000494:pharmacology*; D010446:Peptide Fragments / Q000737:chemistry / Q000494:pharmacology*; D059004:Topoisomerase I Inhibitors; D059005:Topoisomerase II Inhibitors
D004791:Enzyme Inhibitors; D009588:Nitrogen Mustard Compounds; D010446:Peptide Fragments; D059004:Topoisomerase I Inhibitors; D059005:Topoisomerase II Inhibitors; C053654:lexitropsin; D009429:Netropsin; D004264:DNA Topoisomerases, Type I; D004250:DNA Topoisomerases, Type II