A series of novel bichalcones linked with a 1,4-dimethylenepiperazine moiety were prepared and tested for cytotoxicity, with compounds 3 and 4 displaying significant cytotoxicity against all tested tumor cell lines, indicating their potential as anticancer lead drugs.

Chemical & pharmaceutical bulletin

The chalcone basic skeleton is a unique template which is associated with widespread biological activities. In the present study, a series of novel bichalcones linked with a 1,4-dimethylenepiperazine moiety was prepared through Mannich reaction and Clasien-Schmidt condensation. The synthetic analogs 2-16 were subjected into the cytotoxicity examinations using a panel of 25 human tumor cell lines. Among the tested compounds, 3 and 4 which possessed the 3-pyridyl and phenyl groups as the substructure, respectively, displayed significant cytotoxicity against all the tumor cell lines. The results suggested that these bichalcones were potential to be the anticancer lead drugs.

A series of novel bichalcones linked with a 1,4-dimethylenepiperazine moiety were prepared and tested for cytotoxicity, with compounds 3 and 4 displaying significant cytotoxicity against all tested tumor cell lines, indicating their potential as anticancer lead drugs.

Preparation of a series of novel bichalcones linked with a 1,4-dimethylenepiperazine moiety and examination of their cytotoxicity.