|
KMID : 0043319980210020164
|
|
Archives of Pharmacal Research
1998 Volume.21 No. 2 p.164 ~ p.167
|
|
|
Conformationally Constrained Analogues of Diacylglycerol Having a Perhydrofuro[3,4-c]furan-1,4-dione Bis-r-butyrolactone Skeleton
|
|
Lee Jee-Woo
Lewin Nancy-E.
Blumberg Peter-M.
Marquez Victor-E.
|
|
|
Abstract
|
|
|
|
Bis--lactones (1,2) having a perhydrofuro[3,4-c]furan-1,4-dione skeleton were designed as conformationally constrained diacylglycerol analogues. They were synthesized from D-apiose in 11 steps, and evaluated as ligands by measuring their ability to displace bound ]PDBU from the enzyme. The compounds showed moderate binding affinities with values of 13.89 () and 11.47 () , respectively. Their similar binding affinities indicate that these two bicyclic compounds were not effectively discriminated by in terms of the direction of the side chain as other ligands built on similar bis--lactones.
|
|
|
KEYWORD
|
|
|
Protein kinase C, Ligand, Diacylglycerol, Phorbol ester, Bis-r-butyrolactone
|
|
|
FullTexts / Linksout information
|
|
|
|
|
|
Listed journal information
|
|
  
|