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 [3H]thymidine, when compared to non-acetylated analogues.

Graphical abstractPer-O-acetylated-N-glucosyl-thiophene-2-carboxamides showed significant inhibition of both serum and bFGF stimulated uptake of [3H]thymidine, when compared to the unprotected analoguesFigure optionsDownload full-size imageDownload as PowerPoint slide