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Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Synthesis and Antiproliferative and Metabolic Evaluations of Novel Securinine Derivatives
Marc Perez1, Tahar Ayad1, Philippe Maillos2
1PSL Research University, Chimie ParisTech - CNRS, Institut de Recherche de Chimie Paris , 75005 Paris, France.
Abstract:
New securinine analogues have been prepared by semisynthesis. Two series were developed using either Suzuki or Sonogashira cross coupling reactions. The in vitro cytotoxicity of the compounds was assayed against HCT-116 colon cancer cells. The most potent derivatives showed promising growth inhibition on four tumoral cell lines giving a valuable insight on the structure-activity relationship (SAR) of securinine. Moreover, high antiproliferative effect against A-375 (melanoma) was observed with IC50 up to 60 nM.
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