beta-Carbolinedione derivatives as topoisomerase I inhibitors. |
| |
| Authors: | S Mahboobi S Eluwa S Kumar M Koller K St?rl |
| |
| Affiliation: | Institut für Pharmazie, Naturwissenschaftliche Fakult?t IV-Chemie und Pharmazie, Universit?t, Regensburg, Germany. |
| |
| 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. |
| |
| Keywords: | |
|
|
