Orally Active Fumagillin Analogues: Transformations of a Reactive Warhead in the Gastric Environment

[Image: see text] Semisynthetic analogues of fumagillin, 1, inhibit methionine aminopeptidase-2 (MetAP2) and have entered the clinic for the treatment of cancer. An optimized fumagillin analogue, 3 (PPI-2458), was found to be orally active, despite containing a spiroepoxide function that formed a co...

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Detalhes bibliográficos
Main Authors: Arico-Muendel, Christopher C., Blanchette, Heather, Benjamin, Dennis R., Caiazzo, Teresa M., Centrella, Paolo A., DeLorey, Jennifer, Doyle, Elisabeth G., Johnson, Steven R., Labenski, Matthew T., Morgan, Barry A., O’Donovan, Gary, Sarjeant, Amy A., Skinner, Steven, Thompson, Charles D., Griffin, Sarah T., Westlin, William, White, Kerry F.
Formato: Artigo
Idioma:Inglês
Publicado em: American Chemical Society 2013
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC4027436/
https://ncbi.nlm.nih.gov/pubmed/24900682
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/ml3003633
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