Method for the synthesis of flavonoid nitrogen mustard derivatives.

We have prepared a kind of new type of flavonoid nitrogen mustard derivatives with broad-spectrum antitumor activity, which have not been reported in the literature. In the process of preparing intermediate (the flavonoid diethanolamine derivatives) of the target compound, we found that the reasonable separation method is silica gel column chromatography with eluent (MeOH/CHCl, 1:40). The experimental results show that the composition of eluent is an important factor to get high yield of the intermediate, which will directly affect the final yield of the target compound.

Synthesis of flavonoids nitrogen mustard derivatives and study on their antitumor activity in vitro.

Several novel flavonoids nitrogen mustard derivatives were synthesized and evaluated for antiproliferative activity against seven human cancer cell lines (HeLa, A549, HepG2, MCF7, SH-SY5Y, PC-3, DU145) by the MTT assay in vitro. The resulting IC showed that most compounds exhibited better inhibitory activity against seven cell lines. IC values of some compounds were lower than well-known melphalan.