Approach

Challenge & Solution

The design of MTDLs is tough work. Clearly, the yield can be greatly increased by properly selecting the lead compound. Inspired by this concept, chalcones, which already showed broad spectrum of biological activities related to AD, were selected as the lead compound or structure. Chalcones are natural products characterized by the presence of the 1,3-diphenylpropenone structure.  Various experiments demonstrate that chalcones have antioxidant, anti-inflammatory, anti-β-amyloid, and metal-chelating properties.  All these properties are critical in the pathogenesis of AD. 

We rationally designed the synthesis of a series of analogues as multifunctional agents for the treatment of AD.  The chalcone derivatives will be coupled to c-dots and their biological properties will be tested.