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Issue 11, 2005
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Synthesis and biological evaluation of novel fumagillin and ovalicin analogues

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Abstract

A promising approach among the numerous efforts to cure cancer is the interruption of the tumour-induced formation of new blood vessels (angiogenesis). By suppressing angiogenesis with drugs, the tumour can neither grow to a life threatening size, nor metastasize. The natural product fumagillin 1 and the structurally related ovalicin 2 are two of the most potent anti-angiogenic compounds. Here, we report the design and synthesis of novel fumagillin and ovalicin analogues lacking reactive epoxy functionalities, which were thought to be responsible for the severe toxic side-effects observed. We also report a new synthetic approach and the determination of the anti-angiogenic properties of these compounds in endothelial cells.

Graphical abstract: Synthesis and biological evaluation of novel fumagillin and ovalicin analogues

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Publication details

The article was received on 03 Mar 2005, accepted on 13 Apr 2005 and first published on 22 Apr 2005


Article type: Paper
DOI: 10.1039/B503163J
Citation: Org. Biomol. Chem., 2005,3, 2150-2154
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    Synthesis and biological evaluation of novel fumagillin and ovalicin analogues

    R. Mazitschek, A. Huwe and A. Giannis, Org. Biomol. Chem., 2005, 3, 2150
    DOI: 10.1039/B503163J

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