Dysidiolide and related γ-hydroxy butenolide compounds as inhibitors of the protein tyrosine phosphatase, CDC25

Synthetic dysidiolide, as well as several related compounds containing a γ-hydroxybutenolide moiety, were tested in in vitro Cdc25 assays against both synthetic and natural substrates. Contrary to literature values which are in the low micromolar range, we observe only millimolar inhibitory activity...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 1999-09, Vol.9 (17), p.2537-2538
Hauptverfasser:	Blanchard, Jill L., Epstein, David M., Boisclair, Michael D., Rudolph, Johannes, Pal, Kollol
Format:	Artikel
Sprache:	eng
Schlagworte:	4-Butyrolactone - analogs & derivatives 4-Butyrolactone - chemistry 4-Butyrolactone - pharmacology Antineoplastic agents Biological and medical sciences cdc25 Phosphatases - antagonists & inhibitors Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacology General aspects Medical sciences Pharmacology. Drug treatments
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Zusammenfassung:	Synthetic dysidiolide, as well as several related compounds containing a γ-hydroxybutenolide moiety, were tested in in vitro Cdc25 assays against both synthetic and natural substrates. Contrary to literature values which are in the low micromolar range, we observe only millimolar inhibitory activity for these compounds versus Cdc25 phosphatase.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(99)00431-X