beta-Carbolinedione derivatives as topoisomerase I inhibitors.
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.
Mahboobi
S
S
Institut für Pharmazie, Naturwissenschaftliche Fakultät IV-Chemie und Pharmazie, Universität, Regensburg, Germany.
Eluwa
S
S
Kumar
S
S
Koller
M
M
Störl
K
K
D002243:Carbolines / Q000138:chemical synthesis* / Q000494:pharmacology; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D059004:Topoisomerase I Inhibitors
D002243:Carbolines; D004791:Enzyme Inhibitors; D059004:Topoisomerase I Inhibitors