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Identification of Novel Matrix Metalloproteinase Inhibitors by Screening of Phenol Fragments Library
Author(s) -
Rubino Maria Teresa,
Maggi Dariana,
Laghezza Antonio,
Loiodice Fulvio,
Tortorella Paolo
Publication year - 2011
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.201000350
Subject(s) - chemistry , matrix metalloproteinase , phenols , antioxidant , polyphenol , selectivity , matrix metalloproteinase inhibitor , gelatinase , pharmacology , biochemistry , combinatorial chemistry , stereochemistry , biology , catalysis
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.