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Detection of Functional Matrix Metalloproteinases by Zymography
Published on: November 9, 2010
alpha-Amino-beta-sulphone hydroxamates as potent MMP-13 inhibitors that spare MMP-1
D P Becker1, T E Barta, L Bedell
1Departments of Medicinal Chemistry and Inflammation-Oncology, Pharmacia Research & Development, 4901 Searle Parkway, Skokie, IL 60077, USA. daniel.p.becker@pharmacia.com
Bioorganic & Medicinal Chemistry Letters
|October 10, 2001
Abstract:
A series of alpha-amino-beta-sulphone hydroxamates was prepared and evaluated for potency versus MMP-13 and selectivity versus MMP-1. Various substituents were employed on the alpha-amino group (P(1) position), as well as different groups attached to the sulphone group extending into P(1)'. Low nanomolar potency was obtained for MMP-13 with selectivity versus MMP-1 of >1000x for a number of analogues.

