Author/Authors :
Cédrik Garino، نويسنده , , Frédéric Bihel، نويسنده , , Nicolas Pietrancosta، نويسنده , , Younes Laras، نويسنده , , Gilles Quéléver، نويسنده , , Irene Woo، نويسنده , , Peter Klein، نويسنده , , Jenny Bain، نويسنده , , Jean-Luc Boucher، نويسنده , , Jean-Louis Kraus، نويسنده ,
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 α-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
