Chapter 2 - An Overview of Synthetic and Semisynthetic Flavonoid Derivatives and Analogues: Perspectives in Drug Discovery

Abstract

Abstract As a result of their outstanding structural diversity, flavonoids are known to exhibit a wide range of pharmacological properties, including antioxidant, antitumor, antimicrobial, antiinflammatory, antineurodegenerative, and estrogenic. In recent decades a plethora of synthetic and semisynthetic derivatives have been reported in the literature in an attempt to improve the biochemical and pharmacological properties of natural corresponding compounds. Some key structural features and other aspects regarding the interactions of these derivatives with critical cell-signaling pathways and molecular targets associated with various diseases are thoroughly discussed in this chapter. These include: tubulin, topoisomerase, protein kinases (with implications in cancer treatment); HIV integrase; aldose reductase and α-glucosidase (involved in diabetic complications); prostaglandins (which play a role in inflammatory diseases); and acetylcholinesterase and butyrylcholinesterase (involved in Alzheimer's disease). The flavonoid scaffold has represented a remarkable template for the development of numerous compounds with very diverse biological properties. This chapter reviews the biological properties of flavonoid synthetic and semisynthetic derivatives correlated with some key structural features. The chapter attempts to provide support for the future development of synthetic and semisynthetic flavonoid derivatives as potential drugs.