Anhydride modified cantharidin analogues. Is ring opening important in theinhibition of protein phosphatase 2A?

Authors
McCluskey, A Keane, MA Mudgee, LM Sim, ATR Sakoff, J Quinn, RJ
Citation
A. Mccluskey et al., Anhydride modified cantharidin analogues. Is ring opening important in theinhibition of protein phosphatase 2A?, EUR J MED C, 35(10), 2000, pp. 957-964
Citations number
35
Categorie Soggetti
Chemistry & Analysis
Journal title
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
ISSN journal
02235234 → ACNP
Volume
35
Issue
10
Year of publication
2000
Pages
957 - 964
Database
ISI
SICI code
0223-5234(200010)35:10<957:AMCAIR>2.0.ZU;2-9
Abstract
A series of anhydride modified cantharidin analogues have been synthesised and screened for their ability to inhibit protein phosphatase 2A. Surprisin gly only analogues capable of undergoing a facile ring opening of the anhyd ride moiety displayed any significant inhibition. Subsequent NMR experiment s indicated that 7-oxobicyclo[2.2.1]heptane-2,3-dicarboxylic acid was the m ajor (sole) species under assay conditions. The ability of these modified a nhydro-cantharidin analogues to inhibit protein phosphatase 2A varies from 4 (16) to 100% (8) at 100 muM test concentration. (C) 2000 Editions scienti fiques et medicales Elsevier SAS.