2. Academic Validation
  3. Discovery of potent and selective succinyl hydroxamate inhibitors of matrix metalloprotease-3 (stromelysin-1)

Discovery of potent and selective succinyl hydroxamate inhibitors of matrix metalloprotease-3 (stromelysin-1)

  • Bioorg Med Chem Lett. 2001 Feb 26;11(4):571-4. doi: 10.1016/s0960-894x(00)00720-4.
M J Fray 1,  R P Dickinson
Affiliations

Affiliation

  • 1 Department of Discovery Chemistry, Pfizer Global Research and Development, Sandwich, Kent, UK. [email protected]
PMID: 11229774 DOI: 10.1016/s0960-894x(00)00720-4
Abstract

Structure activity relationships are described for a series of succinyl hydroxamic acids 4a-o as potent and selective inhibitors of matrix metalloprotease-3 (stromelysin-1). Optimisation of P1' and P3' groups gave compound 4j (MMP-3 IC50=5.9nM) which was >140-fold less potent against MMP-1 (IC50=51,000nM), MMP-2 (IC50=1790nM), MMP-9 (IC50=840nM) and MMP-14 (IC50=1900nM).

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