β-Carbolinedione Derivatives as Topoisomerase I Inhibitors

Pyrrolo[3,4‐c]‐β‐carbolinedione dimers 5—14 were synthesized from furo[3,4‐c]‐β‐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...

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Published inArchiv der Pharmazie (Weinheim) Vol. 332; no. 7; pp. 249 - 254
Main Authors Mahboobi, Siavosh, Eluwa, Stella, Kumar KC, Sunil, Koller, Markus, Störl, Karin
Format Journal Article
LanguageEnglish
Published Weinheim WILEY-VCH Verlag GmbH 01.07.1999
WILEY‐VCH Verlag GmbH
Wiley-VCH
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Summary:Pyrrolo[3,4‐c]‐β‐carbolinedione dimers 5—14 were synthesized from furo[3,4‐c]‐β‐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]‐β‐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.
Bibliography:ark:/67375/WNG-70VHJC7B-2
istex:7C3676DB967B1E09CA804150CEDACD46E7CCDFC0
ArticleID:ARDP249
ObjectType-Article-1
SourceType-Scholarly Journals-1
ObjectType-Feature-2
content type line 23
ISSN:0365-6233
1521-4184
DOI:10.1002/(SICI)1521-4184(19997)332:7<249::AID-ARDP249>3.0.CO;2-F