Information from the abstract
Three new scortechinone D derivatives ( 2 – 4 ) were effectively obtained through in situ halogenation of scortechinone D ( 1 ) using Oxone and sodium halide in a mixture of acetonitrile and water (5:1 ratio). All compounds were characterized using 1D and 2D NMR spectroscopy and high-resolution mass spectrometry. Single crystal-XRD was successfully performed on the compound 4 possessing iodo group at C-17. Among the four compounds ( 1 – 4 ) tested, compound 2 showed good inhibitory activity against EGFR tyrosine kinase with an inhibition value of 63.5% at 10 μM and modest toxicity against WI-38 normal cell line with 58.8% growth suppression at the same concentration. Despite the considerable toxicity of the active compound, this discovery offers a novel insight into the reactivity and bioactivity of scortechinone D analogs.
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Related topics: HER2/EGFR in Cancer Research · Protein Tyrosine Phosphatases · Synthesis of Organic Compounds
Thai researcher and institutional participation
Sutin Kaennakam · Warinthorn Chavasiri · King Mongkut's University of Technology North Bangkok · Chulalongkorn University
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