Thai chemists used Oxone and sodium halides for late-stage halogenation of scortechinone D, yielding three new derivatives characterised by NMR/HRMS and X-ray for the iodo compound. Compound 2 inhibited EGFR tyrosine kinase by 63.5% at 10 μM but also suppressed normal WI-38 cell growth by 58.8% at the same concentration, indicating poor selectivity and no drug-ready lead.
Key findings
- Three new derivatives were obtained, and the iodo structure was confirmed crystallographically. Of four tested compounds, compound 2 gave 63.5% EGFR inhibition at 10 μM but 58.8% WI-38 growth suppression at the same concentration. No IC50, cellular target engagement or selectivity index was reported.
Why this matters globally
Late-stage functionalisation expands natural-product chemical space without rebuilding the core and can accelerate lead discovery. Cancer relevance requires potency, selectivity, mechanism and pharmacology through many further stages.
Thai researcher contribution
KMUTNB and Chulalongkorn University combined reaction chemistry, structural elucidation and biological screening of a natural-product scaffold.
Limitations to consider
Only three new derivatives and a single screening concentration were used. The active compound's normal-cell toxicity approached its inhibition level. No cancer panel, mutant EGFR, kinase selectivity, metabolism, solubility or animal work was reported. Enzyme inhibition is not therapeutic efficacy.