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ID: ALA1134078
Journal: Bioorg Med Chem Lett
Title: Structure-based design, synthesis and SAR of a novel series of thiopheneamidine urokinase plasminogen activator inhibitors.
Authors: Subasinghe NL, Illig C, Hoffman J, Rudolph MJ, Wilson KJ, Soll R, Randle T, Green D, Lewandowski F, Zhang M, Bone R, Spurlino J, DesJarlais R, Deckman I, Molloy CJ, Manthey C, Zhou Z, Sharp C, Maguire D, Crysler C, Grasberger B.
Abstract: The serine protease urokinase plasminogen activator (uPA) is thought to play a central role in tumor metastasis and angiogenesis. Molecular modeling studies suggest that 5-thiomethylthiopheneamidine inhibits uPA by binding at the S1 pocket of the active site. Further structure based elaboration of this residue resulted in a novel class of potent and selective inhibitors of uPA.
CiteXplore: 11378359