title: 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.
authors.affiliation: Dipartimento Farmaco-Chimico, Università degli Studi "Aldo Moro", Bari, Italy.
authors.forename: Maria Teresa
authors.initials: MT
authors.lastname: Rubino
authors.forename: Dariana
authors.initials: D
authors.lastname: Maggi
authors.forename: Antonio
authors.initials: A
authors.lastname: Laghezza
authors.forename: Fulvio
authors.initials: F
authors.lastname: Loiodice
authors.forename: Paolo
authors.initials: P
authors.lastname: Tortorella
mesh_terms: D015195:Drug Design; D004353:Drug Evaluation, Preclinical; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D006801:Humans; D061965:Matrix Metalloproteinase Inhibitors; D020782:Matrix Metalloproteinases / Q000378:metabolism; D058990:Molecular Targeted Therapy; D059808:Polyphenols; D054852:Small Molecule Libraries
chemical_list: D004791:Enzyme Inhibitors; D061965:Matrix Metalloproteinase Inhibitors; D059808:Polyphenols; D054852:Small Molecule Libraries; D020782:Matrix Metalloproteinases