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Published on: February 9, 2021
New 2-bromomethyl-8-substituted-benzo[c]chromen-6-ones. Synthesis and biological properties
Cédrik Garino1, Frédéric Bihel, Nicolas Pietrancosta
1Laboratoire de Chimie Biomoléculaire, Unité INSERM U-623-IBDM, Département de Chimie, Faculté des Sciences Luminy, Université de La Méditerranée, 13288 Marseille cedex 9, France.
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.
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