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ID: ALA1145141
Journal: Bioorg Med Chem Lett
Title: New 2-bromomethyl-8-substituted-benzo[c]chromen-6-ones. Synthesis and biological properties.
Authors: Garino C, Bihel F, Pietrancosta N, Laras Y, Quéléver G, Woo I, Klein P, Bain J, Boucher JL, Kraus JL.
Abstract: New 2-bromomethyl-8-substituted-benzo[c]chromen-6-ones have been synthesized and their bioactive properties have been evaluated on different enzymatic models: serine proteases (trypsin and alpha-chymotrypsin), HIV aspartyl protease, nitric oxide synthase and a panel of protein kinases. These new derivatives can provide upon chemical or enzymatic attack, very reactive quinonimine methide intermediates, which could be utilized for the design of enzyme inhibitors. We found that some of these new derivatives exhibit modest inhibitory activities on the studied enzyme models, but it could be improved after structure optimization.
CiteXplore: 15582426