N-Glycosyl-thiophene-2-carboxamides: effects on endothelial cell growth in the presence and absence of bFGF--a significant increase in potency using per-O-acetylated sugar analogues.
Inhibitors of endothelial cell proliferation are of interest in development of therapies for angiogenesis related disease. N-Glucosyl-thiophene-2-carboxamides have been synthesized and evaluated for their effects on proliferation in bovine aortic endothelial cells. Per-O-acetylated-N-glucosyl-thiophene-2-carboxamides showed improved inhibition of both serum and bFGF stimulated uptake of [(3)H]thymidine, when compared to non-acetylated analogues.
Rawe
Sarah L
SL
Centre for Synthesis and Chemical Biology, UCD School of Chemistry and Chemical Biology, UCD Conway Institute, University College Dublin, Belfield, Dublin 4, Ireland.
Zaric
Violeta
V
O'Boyle
Kathy M
KM
Murphy
Paul V
PV
D000107:Acetylation; D000577:Amides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D000818:Animals; D002241:Carbohydrates / Q000737:chemistry*; D002417:Cattle; D049109:Cell Proliferation / Q000187:drug effects; D002478:Cells, Cultured; D042783:Endothelial Cells / Q000166:cytology* / Q000187:drug effects*; D016222:Fibroblast Growth Factor 2 / Q000494:pharmacology*; D006031:Glycosylation; D015394:Molecular Structure; D013876:Thiophenes / Q000737:chemistry*
D000577:Amides; D002241:Carbohydrates; D013876:Thiophenes; D016222:Fibroblast Growth Factor 2