Synthesis and biological evaluation of chalcone and stilbene based acetamidines as nitric oxide synthase inhibitors

Nitric Oxide Synthases (NOS) are a family of oxidoreductases responsible for the biosynthesis of the free radical nitric oxide (NO). This is a very important signalling molecule involved in many different biological processes, both physiologic and pathologic.

In particular, the inhibition of the inducible NOS (iNOS) has been proposed as a targeted therapy in several diseases, including cancer, neurodegeneration and inflammatory bowel disease. In the past years our research group has disclosed different new potent and selective acetamidines as iNOS inhibitors, collecting evidence their usefulness as anticancer agents.

In the present work, starting from the observation that different chalcone-based compounds can modulate the iNOS expression levels, we have synthesised a set of acetamidin-chalcones and acetamidin-stilbenes and we evaluated them as inhibitors of the iNOS activity. Results obtained from these studies will be presented.