su-11248 and Diabetic-Retinopathy

Diabetic retinopathy is the leading cause of blindness which is associated with excessive angiogenesis. Using the structure of wondonin marine natural products, we previously created a scaffold to develop a novel type of antiangiogenesis agent that possesses minimized cytotoxicity. To overcome its poor pharmaceutical properties, we further modified the structure. A new scaffold was derived in which the stereogenic carbon was changed to nitrogen and the 1,2,3-triazole ring was replaced by an alkyl chain. By comparing the bioactivity versus cytotoxicity, compound

Topics: Angiogenesis Inhibitors; Angiopoietin-2; Animals; Cell Survival; Diabetic Retinopathy; Disease Models, Animal; Down-Regulation; Drug Design; Drug Stability; Glucose; Human Umbilical Vein Endothelial Cells; Humans; Mice; Mice, Inbred C57BL; Neovascularization, Physiologic; Phosphatidylinositol 3-Kinases; Signal Transduction; Small Molecule Libraries; Structure-Activity Relationship; Triazoles