药物化学

Synthesis and Evaluation of Anticancer Activity of O-allylchalcone Derivatives

Abstract

Bathélémy Ngameni, Victor Kuete, Pantaleon Ambassa, kamga Justin, Moungang Luciane Marlyse, Abdou Tchoukoua, René Roy, Bonaventure Tchaleu Ngadjui and Murayama Tetsuya

A large number of novel O -allylchalcones were synthesized by Claisen Schmidt condensation reaction of O -allylvanillin 3 with appropriate substituted acetophenones 4a-h. These model chalcones 5a-h and their precursor O -allylvanillin were screened for their in vitro cytotoxicactivity against four human cancer cell lines. The most potent compound in this series with the IC 50 values below or around 10 μM were 5f against THP-1 cells (10.42 μM) and 5g against THP-1 (4.76 μM), DU-145 (5.21 μM), HL60 (7.90 μM), Hep-G2 (10.12 μM) and MCF-7 (10.32 μM).