Design, synthesis, and evaluation of a water soluble C5-monoketone type curcumin analogue as a potent amyloid beta aggregation inhibitor

摘要

A structure activity relationship study of curcumin analogues for the inhibition of amyloid beta aggregation is described. Optimization of the o-phenol and olefin spacer resulted in the identification of the C5-monoketone type curcumin analogue AY1319, which exhibited potent anti-amyloid beta aggregation activity (leading to nanorod-like fragments), sufficient water solubility, and low cytotoxicity.