Design and synthesis of naphthylchalcones as novel anti-leukaemia agents.

A series of new hydroxylated chalcone derivatives with different substitution patterns on a phenyl ring A and B, were prepared by Claisen-Schmidt condensation in an aqueous alkaline base. The antiproliferative activity of the studied compounds was evaluated against the human leukaemia cell line U-937. The structure-activity relationship of these naphthylchalcones was investigated by the introduction of one methoxy or two methyl groups on the A ring, the introduction of a methoxy group on the naphthyl ring or by varying the position of the methoxy group on the A ring.

Chalcones: Retrospective Synthetic Approaches and Mechanistic Aspects of a Privileged Scaffold.

This review summarizes the synthetic methodologies used in the last 25 years for the synthesis of chalcones, which are a class of flavonoids having a 1,3-diphenyl-2-propene-1-one backbone. These compounds are considered a hot topic in the field of medicinal chemistry, due to their pharmacological activity and because they are important precursors for the synthesis of heterocyclic compounds with therapeutic applications such as: flavones, flavanones, isoxazolines, benzothiazepines, pyrimidines and pyrazolines derivatives.