| 10658599 |
Laidley CW, Dauben WG, Guo ZR, Lam JY, Casida JE: 2-Carboxymethylendothal analogues as affinity probes for stabilized protein phosphatase 2A. Bioorg Med Chem. 1999 Dec;7(12):2937-44.
Endothal (1diacid) and [3H] cantharidic acid ([3H] CA) bind with high affinity to the catalytic subunit of protein phosphatase 2A (PP2A). PP2A in liver cytosol was greatly stabilized with 30% glycerol as a preliminary step in the potential use of endothal-type derivatives for affinity chromatography. We report here the first introduction of a functionalizable group into endothal which allows retention of binding site affinity (assayed as [3H] CA binding in mouse liver cytosol). 2-Carboxymethylendothal anhydride (7) was prepared in two steps and 97% overall yield from cis-aconitic anhydride and furan. The potency of 7 was retained on conversion to two 2-carboxymethyl esters but not to two 2-(n-alkylcarboxamidomethyl) analogues. |
62(0,2,2,2) |