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Issue 24, 2008
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Design, synthesis and biological evaluation of bridged epothilone D analogues

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Abstract

Six epothilone D analogues with a bridge between the C4-methyl and the C12-methyl carbons were prepared in an attempt to constrain epothilone D to its proposed tubulin-binding conformation. Ring-closing metathesis (RCM) was employed as the key step to build the C4–C26 bridge. In antiproliferative assays in the human ovarian cancer (A2780) and prostate cancer (PC3) cell lines, and also in tubulin assembly assay, all these compounds proved to be less active than epothilone D.

Graphical abstract: Design, synthesis and biological evaluation of bridged epothilone D analogues

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Publication details

The article was received on 26 Aug 2008, accepted on 26 Sep 2008 and first published on 06 Nov 2008


Article type: Paper
DOI: 10.1039/B814823F
Citation: Org. Biomol. Chem., 2008,6, 4542-4552
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    Design, synthesis and biological evaluation of bridged epothilone D analogues

    Q. Chen, T. Ganesh, P. Brodie, C. Slebodnick, Y. Jiang, A. Banerjee, S. Bane, J. P. Snyder and D. G. I. Kingston, Org. Biomol. Chem., 2008, 6, 4542
    DOI: 10.1039/B814823F

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