Structure-Based design, synthesis and SAR of a novel series of thiopheneamidine urokinase plasminogen activator inhibitors

Nalin L. Subasinghe, Carl Illig, James Hoffman, M. J. Rudolph, Kenneth J. Wilson, Richard Soll, Troy Randle, David Green, Frank Lewandowski, Marie Zhang, Roger Bone, John Spurlino, Renee DesJarlais, Ingrid Deckman, Christopher J. Molloy, Carl Manthey, Zhau Zhou, Celia Sharp, Diane Maguire, Carl CryslerBruce Grasberger

Research output: Contribution to journalArticle

14 Scopus citations

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.

Original languageEnglish (US)
Pages (from-to)1379-1382
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume11
Issue number11
DOIs
StatePublished - Jun 4 2001
Externally publishedYes

All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

Fingerprint Dive into the research topics of 'Structure-Based design, synthesis and SAR of a novel series of thiopheneamidine urokinase plasminogen activator inhibitors'. Together they form a unique fingerprint.

  • Cite this

    Subasinghe, N. L., Illig, C., Hoffman, J., Rudolph, M. J., Wilson, K. J., Soll, R., Randle, T., Green, D., Lewandowski, F., Zhang, M., Bone, R., Spurlino, J., DesJarlais, R., Deckman, I., Molloy, C. J., Manthey, C., Zhou, Z., Sharp, C., Maguire, D., ... Grasberger, B. (2001). Structure-Based design, synthesis and SAR of a novel series of thiopheneamidine urokinase plasminogen activator inhibitors. Bioorganic and Medicinal Chemistry Letters, 11(11), 1379-1382. https://doi.org/10.1016/S0960-894X(01)00247-5