8,9-Methylenedioxybenzo[i]phenanthridines_ Topoisomerase I-Targeting activity and cytotoxicity
Substituted benzo[i]phenanthridines that have incorporated within their structure an 8,9-methylenedioxy group can exhibit topoisomerase I-targeting activity. Structure–activity studies were performed to examine the influence of saturation at the 11,12-positions of several substituted 8,9-methylenedi...
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| Main Authors: | , , , , , , |
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| Format: | Article |
| Language: | English |
| Published: |
Elsevier Ltd
2003
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| Subjects: | |
| Online Access: | http://ir.unimas.my/id/eprint/2199/1/Bioorganic.pdf http://ir.unimas.my/id/eprint/2199/ http://www.sciencedirect.com/science/article/pii/S0968089603003948 |
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| Summary: | Substituted benzo[i]phenanthridines that have incorporated within their structure an 8,9-methylenedioxy group can exhibit topoisomerase I-targeting activity. Structure–activity studies were performed to examine the influence of saturation at the 11,12-positions of several substituted 8,9-methylenedioxybenzo[i]phenanthridines. The activities of these dihydro analogues were compared to those of their unsaturated analogues. In addition, the influence of varying substituents at the 2- and 3-positions within the A-ring of these 8,9-methylenedioxybenzo[i]phenanthridines on their relative potency as topoisomerase I-targeting agents and cell proliferation as determined using the MTT assay was investigated. 2,3-Dimethoxy-8,9 Methylenedioxybenzo[i]phenanthridine and its 11,12-dihydro derivative were among the more potent analogues evaluated with regard to topoisomerase I-targeting activity and cytotoxicity. |
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