Novel thiol-based TACE inhibitors: Rational design, synthesis, and SAR of thiol-containing aryl sulfonamides
Copyright policy )Novel thiol-based TACE inhibitors: Rational design, synthesis, and SAR of thiol-containing aryl sulfonamides
A series of potent thiol-containing aryl sulfonamide TACE inhibitors was designed and synthesized. The SAR and MMP selectivity of the series were investigated. In particular, compound 4b has shown excellent in vitro potency against the isolated TACE enzyme and good selectivity over MMP-2, -7, -8, -9, and -13. The X-ray structure of 4b bound to TACE was obtained.
- Vertex Pharmaceuticals (United States) United States
Sulfonamides, ADAM17 Protein, Substrate Specificity, Arthritis, Rheumatoid, ADAM Proteins, Structure-Activity Relationship, Crohn Disease, Drug Design, Metalloproteases, Humans, Sulfhydryl Compounds, Enzyme Inhibitors
Sulfonamides, ADAM17 Protein, Substrate Specificity, Arthritis, Rheumatoid, ADAM Proteins, Structure-Activity Relationship, Crohn Disease, Drug Design, Metalloproteases, Humans, Sulfhydryl Compounds, Enzyme Inhibitors
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