8,9-Methylenedioxybenzo[i]phenanthridines_ Topoisomerase I-Targeting activity and cytotoxicity

Li, D. and Zhao, B. and Sim, S.P and Li, T.K and Liu, A. and Liu, L.F. and LaVoie, E.J. (2003) 8,9-Methylenedioxybenzo[i]phenanthridines_ Topoisomerase I-Targeting activity and cytotoxicity. Bioorganic & Medicinal Chemistry, 11 (17). pp. 3795-3805.

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Abstract

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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