3-O-Substituted-3',4',5'-trimethoxyflavonols: Synthesis and cell-based evaluation as anti-prostate cancer agents.

摘要: Abstract Twenty-two 3- O -substituted-3′,4′,5′-trimethoxyflavonols have been designed and synthesized for their anti-proliferative activity towards three human prostate cancer cell lines. Our results indicate that most of them are significantly more potent than the parent 3′,4′,5′-trimethoxyflavonol in inhibiting proliferation PC-3 LNCaP models. -Substituted-3′,4′,5′-trimethoxyflavonols generally higher potency lines DU145 line. Incorporation an ethyl group to 3-OH leads -ethyl-3′,4′,5′-trimethoxyflavonol as optimal derivative with up 36-fold enhanced compared corresponding lead compound 3′,4′,5′-trimethoxyflavonol, but reversed apoptotic response. Introduction a dipentylaminopropyl increases not only antiproliferative also ability activating apoptosis. findings imply modification on trimethoxyflavonol can further enhance its vitro apoptosis induction.