Title of article
Phosphinic acid-based MMP-13 inhibitors that spare MMP-1 and MMP-3
Author/Authors
Lawrence A. Reiter، نويسنده , , Peter G. Mitchell، نويسنده , , Gary J. Martinelli، نويسنده , , Lori L. Lopresti-Morrow، نويسنده , , Sue A. Yocum، نويسنده , , James D. Eskra، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2003
Pages
6
From page
2331
To page
2336
Abstract
Phosphinic acid-based inhibitors of MMP-13 have been investigated with the aim of identifying potent inhibitors with high selectivity versus MMP-1. Independent variation of the substituents on a P1′ phenethyl group and a P2 benzyl group improved potencies in both cases around 3-fold over the unsubstituted parent. Combining improved P1′ and P2 groups into a single molecule gave an inhibitor with a 4.5 nM IC50 against MMP-13 and which is 270-fold selective over MMP-1.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2003
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
793350
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