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Issue 39, 2012
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Synthesis and biological evaluation of novel isoellipticine derivatives and salts

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Abstract

Synthesis of novel 7-substituted isoellipticines and isoellipticinium salts is described, with optimisation of routes, representing a new class of anti-cancer agent. Initial assessment of biological activity using a topoisomerase II decatenation assay and NCI screening highlighted strong anti-cancer activity, further developed in a panel of isoellipticinium salts. Interestingly, low correlation between results of the topoisomerase II decatenation assay and NCI screen throughout the panel suggest that topo II is not the most important biological target with respect to anti-cancer activity in this new class of compounds. Results also suggest that solubility is not the limiting factor in activity of the isoellipticinium salts. Overall, 20 novel ellipticine analogues were prepared and full anti-cancer profiling was completed for 13 isoellipticine derivatives and salts. Two compounds display significant specificity towards CNS cancer cell lines and are lead compounds for future development.

Graphical abstract: Synthesis and biological evaluation of novel isoellipticine derivatives and salts

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Publication details

The article was received on 20 Jun 2012, accepted on 24 Aug 2012 and first published on 24 Aug 2012


Article type: Paper
DOI: 10.1039/C2OB26181B
Citation: Org. Biomol. Chem., 2012,10, 7912-7921
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    Synthesis and biological evaluation of novel isoellipticine derivatives and salts

    C. M. Miller, E. C. O'Sullivan, K. J. Devine and F. O. McCarthy, Org. Biomol. Chem., 2012, 10, 7912
    DOI: 10.1039/C2OB26181B

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