1. Synthesis and biological activity of ferrocenyl indeno[1,2-c]isoquinolines as topoisomerase II inhibitors.
- Author
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Wambang N, Schifano-Faux N, Aillerie A, Baldeyrou B, Jacquet C, Bal-Mahieu C, Bousquet T, Pellegrini S, Ndifon PT, Meignan S, Goossens JF, Lansiaux A, and Pélinski L
- Subjects
- Antigens, Neoplasm metabolism, Antineoplastic Agents chemical synthesis, Antineoplastic Agents chemistry, Cell Proliferation drug effects, DNA Topoisomerases, Type II metabolism, DNA-Binding Proteins metabolism, Dose-Response Relationship, Drug, Drug Screening Assays, Antitumor, Ferrous Compounds chemistry, Humans, Inhibitory Concentration 50, Isoquinolines chemistry, Molecular Structure, Structure-Activity Relationship, Topoisomerase II Inhibitors chemistry, Tumor Cells, Cultured, Antineoplastic Agents pharmacology, DNA-Binding Proteins antagonists & inhibitors, Ferrous Compounds chemical synthesis, Ferrous Compounds pharmacology, Isoquinolines chemical synthesis, Isoquinolines pharmacology, Topoisomerase II Inhibitors chemical synthesis, Topoisomerase II Inhibitors pharmacology
- Abstract
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., (Copyright © 2015 Elsevier Ltd. All rights reserved.)
- Published
- 2016
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