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Issue 27, 2016
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Bipiperidine conjugates as soluble sugar surrogates in DNA-intercalating antiproliferative polyketides

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Abstract

DNA-intercalating polyketide glycosides are important leads for cancer therapeutics, yet their use is often limited by their low solubility and challenging synthetic protocols. To overcome these limitations, we employed 1,4′-bipiperidine-1′-carbamate residues as sugar surrogates in daunorubicin and chartreusin, yielding water-soluble derivatives and prodrugs with dramatically improved antiproliferative activities.

Graphical abstract: Bipiperidine conjugates as soluble sugar surrogates in DNA-intercalating antiproliferative polyketides

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Publication details

The article was received on 28 Jan 2016, accepted on 26 Feb 2016 and first published on 26 Feb 2016


Article type: Communication
DOI: 10.1039/C6CC00890A
Chem. Commun., 2016,52, 4894-4897

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    Bipiperidine conjugates as soluble sugar surrogates in DNA-intercalating antiproliferative polyketides

    N. Ueberschaar, F. Meyer, H. Dahse and C. Hertweck, Chem. Commun., 2016, 52, 4894
    DOI: 10.1039/C6CC00890A

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