Identification of Novel Matrix Metalloproteinase Inhibitors by Screening of Phenol Fragments Library

Abstract In the last 20 years, a great variety of synthetic, low molecular weight MMP inhibitors (MMPIs) have been synthesized and tested, although none has reached clinical utility. Exploration of novel ZBGs and development of non‐hydroxamate MMPI has become a focus in current research. It's well‐known that polyphenols can produce beneficial effects on human health by their antioxidant properties as well as they have the ability to block gelatinase activity. In this work we tested a series of selected phenols as MMP inhibitors. The most interesting hit ( B6 ) shows sub‐micromolar activity against MMP‐2 (IC 50 0.59 ± 0.05 µM, LE = 1.07) and a fairly good selectivity spectrum.