Novel thiol-based TACE inhibitors. Part 2: Rational design, synthesis, and SAR of thiol-containing aryl sulfones
Copyright policy )Novel thiol-based TACE inhibitors. Part 2: Rational design, synthesis, and SAR of thiol-containing aryl sulfones
A series of potent thiol-containing aryl sulfone TACE inhibitors were designed and synthesized. The SAR and MMP selectivity of the series were investigated. In particular, compound 8b showed excellent in vitro potency against the isolated enzyme and good selectivity over MMP-2, -7, -8, -9, and -13. The X-ray structure of 8b in complex with TACE was also obtained.
- Vertex Pharmaceuticals (United States) United States
Models, Molecular, Metalloendopeptidases, ADAM17 Protein, Crystallography, X-Ray, Substrate Specificity, Isoenzymes, ADAM Proteins, Kinetics, Structure-Activity Relationship, Drug Design, Protease Inhibitors, Sulfhydryl Compounds, Sulfones
Models, Molecular, Metalloendopeptidases, ADAM17 Protein, Crystallography, X-Ray, Substrate Specificity, Isoenzymes, ADAM Proteins, Kinetics, Structure-Activity Relationship, Drug Design, Protease Inhibitors, Sulfhydryl Compounds, Sulfones
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