title: beta-Carbolinedione derivatives as topoisomerase I inhibitors.
abstract: Pyrrolo[3,4-c]-beta-carbolinedione dimers 5-14 were synthesized from furo[3,4-c]-beta-carbolinediones and diamines by solvent-free TaCl5/silica catalyzed reaction under microwave irradiation. The inhibitory property of these target compounds, the starting materials 2, 31, 32, and the N-alkylated pyrrolo[3,4-c]-beta-carbolinediones 16, 17, 20-30 was tested against the relaxation of supercoiled pRB322 DNA by calf thymus topoisomerases I and II. Some of these compounds, especially 7 and 23 proved to be selective inhibitors of topoisomerase I.
authors.affiliation: Institut für Pharmazie, Naturwissenschaftliche Fakultät IV-Chemie und Pharmazie, Universität, Regensburg, Germany.
authors.forename: S
authors.initials: S
authors.lastname: Mahboobi
authors.forename: S
authors.initials: S
authors.lastname: Eluwa
authors.forename: S
authors.initials: S
authors.lastname: Kumar
authors.forename: M
authors.initials: M
authors.lastname: Koller
authors.forename: K
authors.initials: K
authors.lastname: Störl
mesh_terms: D002243:Carbolines / Q000138:chemical synthesis* / Q000494:pharmacology; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D059004:Topoisomerase I Inhibitors
chemical_list: D002243:Carbolines; D004791:Enzyme Inhibitors; D059004:Topoisomerase I Inhibitors