Potent MMP inhibitor (IC50
values are <0.1, <0.1, 0.18, 1.7, 13 and 28.7 nM for MMP-2, -13, -9, -8, -14 and -3 respectively). Exhibits 100,000-fold selectivity for MMP-2 and -13 over MMP-1. Reduces left ventricular dilation in a myocardial infarction rat model. Orally bioavailable.
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Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.
Becker et al.