Synthesis, biological activity and comparative analysis of DNA binding affinities and human DNA topoisomerase I inhibitory activities of novel 12-alkoxy-benzo[c]phenanthridinium salts - Substances d'Origine Naturelle et Analogues Structuraux Accéder directement au contenu
Article Dans Une Revue Bioorganic and Medicinal Chemistry Letters Année : 2001

Synthesis, biological activity and comparative analysis of DNA binding affinities and human DNA topoisomerase I inhibitory activities of novel 12-alkoxy-benzo[c]phenanthridinium salts

Résumé

New antitumor 12-alkoxy-benzo[c]phenanthridinium derivatives were obtained in high yields through multistep syntheses. Analysis of DNA binding and human DNA topoisomerase I inhibitory activities demonstrates that new compounds, combining 2, 6, and 12 substitutions, interact strongly with DNA and exhibit important topoisomerase I inhibition. The cytotoxicities against solid tumor cell lines are also determined and compared with those for fagaronine and ethoxidine. Synthesis and biological evaluations of new topoisomerase I benzo[c]phenanthridinium salts inhibitors is reported.

Dates et versions

hal-03639024 , version 1 (12-04-2022)

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Michael Lynch, Olivier Duval, Alyona Sukhanova, Jerome Devy, Simon Mackay, et al.. Synthesis, biological activity and comparative analysis of DNA binding affinities and human DNA topoisomerase I inhibitory activities of novel 12-alkoxy-benzo[c]phenanthridinium salts. Bioorganic and Medicinal Chemistry Letters, 2001, 11 (19), pp.2643-2646. ⟨10.1016/S0960-894X(01)00520-0⟩. ⟨hal-03639024⟩
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