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Synthesis and biological activity of ferrocenyl indeno[1,2-c]isoquinolines as topoisomerase II inhibitors

Résumé : Three series of indeno[1,2-c]isoquinolines bearing a ferrocenyl entity were synthesized and evaluated for DNA interaction, topoisomerase I and II inhibition, and cytotoxicity against breast human cancer cell lines. In the first and second series, the ferrocenyl scaffold was inserted as a linker between the two nitrogen atoms. In the last series, it was introduced at the end of the carbon chain. The present study showed that the ferrocenyl entity enhanced the topoisomerase II inhibition. Most compounds showed a potent growth inhibitory effect on MDA-MB-231 cell line with the IC50 in μM range.
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https://hal.univ-lille.fr/hal-03038231
Contributeur : Lilloa Université de Lille <>
Soumis le : jeudi 3 décembre 2020 - 13:33:39
Dernière modification le : vendredi 26 mars 2021 - 17:52:01

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Nathalie Wambang, Nadege Schifano, Alexandre Aillerie, Brigitte Baldeyrou, Camille Jacquet, et al.. Synthesis and biological activity of ferrocenyl indeno[1,2-c]isoquinolines as topoisomerase II inhibitors. Bioorganic and Medicinal Chemistry, Elsevier, 2016, Bioorganic & medicinal chemistry, 24, pp.651-660. ⟨10.1016/j.bmc.2015.12.033⟩. ⟨hal-03038231⟩

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