Abstract: Alzheimer's disease (AD) is the most common chronic progressive neurodegenerative disease in elder people. At present, the pathogenesis of AD is still unclear. Due to the complex pathogenesis of AD, multi-target drugs are an important research direction for AD therapies. In addition, the development of imaging probes targeting amyloid β-protein (Aβ) plaque plays a key role in the early diagnosis of AD. Chalcone is a natural compound with diverse biological activities that deserves further development. According to the current literature, the development of chalcone and its derivatives into multi-target AD therapies and diagnostic Aβ imaging probes was summarized based on their activities on acetycholinesterase (AChE) inhibition, antioxidation, monoamine oxidase B (MAO-B) inhibition, Aβ aggregation inhibition, so as to provide useful information and theoretical basis for AD treatment and diagnosis.