Synthesis and biological evaluation of new securinine analogues as potential anticancer agents

• New securinine derivatives are evaluated for cytotoxicity.
• Compounds bearing a meta substituted aryl moiety are more potent than securinine.
• A 80-fold increase in potency is observed.

A series of new securinine analogues was prepared by Heck reaction from readily accessible securinine and commercially available iodoarenes. The in vitro cytotoxicity of the prepared compounds was assayed against a panel of four cancer cell lines: A375, A549, HCT-116 and HL-60 showing promising growth inhibition with excellent IC50 values in the nanomolar range. The plasmatic stability of the most potent analogue was also investigated demonstrating that they might serve as valuable leads for the development of anticancer drugs.

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