Anthranilate sulfonamide hydroxamate TACE inhibitors. Part 1: Structure-based design of novel acetylenic P1' groups

Bioorg Med Chem Lett. 2002 Apr 22;12(8):1195-8. doi: 10.1016/s0960-894x(02)00135-x.

Abstract

The structure-based design of potent sulfonamide hydroxamate TACE inhibitors bearing novel acetylenic P1' groups has led to compounds with excellent in vitro potency against TACE and selectivity over MMP-1.

MeSH terms

  • ADAM Proteins
  • ADAM17 Protein
  • Acetylene / chemistry*
  • Amino Acid Sequence
  • Enzyme Inhibitors / chemistry*
  • Enzyme Inhibitors / pharmacology*
  • Hydroxamic Acids / chemistry*
  • Hydroxamic Acids / pharmacology*
  • Metalloendopeptidases / antagonists & inhibitors*
  • Models, Molecular
  • Molecular Sequence Data
  • Molecular Structure
  • Sulfonamides / chemical synthesis*
  • Sulfonamides / pharmacology*
  • ortho-Aminobenzoates / chemistry*
  • ortho-Aminobenzoates / pharmacology*

Substances

  • Enzyme Inhibitors
  • Hydroxamic Acids
  • Sulfonamides
  • ortho-Aminobenzoates
  • ADAM Proteins
  • Metalloendopeptidases
  • ADAM17 Protein
  • Acetylene