1 research outputs found
Synthesis and Antiproliferative and Metabolic Evaluations of Novel Securinine Derivatives
New securinine analogues have been
prepared by semisynthesis. Two
series were developed using either Suzuki or Sonogashira cross coupling
reactions. The <i>in vitro</i> 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 IC<sub>50</sub> up to 60 nM