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Organic & biomolecular chemistry DOI:10.1039/b503163j

Synthesis and biological evaluation of novel fumagillin and ovalicin analogues.

Publication TypeJournal Article
Year of Publication2005
AuthorsMazitschek, R, Huwe, A, Giannis, A
JournalOrganic & biomolecular chemistry
Volume3
Issue11
Pages2150-4
Date Published2005/06/07
ISSN1477-0520
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.

URLhttp://dx.doi.org/10.1039/b503163j
DOI10.1039/b503163j
Pubmed

http://www.ncbi.nlm.nih.gov/pubmed/15917904?dopt=Abstract