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

Abstract

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 IC₅₀ showed that most compounds exhibited better inhibitory activity against seven cell lines. IC₅₀ values of some compounds were lower than well-known melphalan. In particular, compound 8b was the most promising compound which inhibited HeLa cells with IC₅₀ value of 1.43 μM. It showed excellent antitumor activity against these seven cell lines. Besides, it could arrest cell cycle of HeLa in G2/M phase and induce cell apoptosis. The loss of mitochondrial membrane potential may be an apoptotic mediating factor.

Keywords: Anticancer; Cell apoptosis; Cell cycle; Flavonoids; Nitrogen mustard derivatives.