A facile
and metal-free one-pot protocol for the synthesis of fused
imidazopyridine scaffolds has been developed. This novel protocol
combines the Groebke–Blackburn–Bienaymé reaction
(GBBR) with a sequential TBAB-mediated cyclization cascade. Biological
evaluation demonstrated that compound 6a inhibits human
prostate cancer cell DU-145 proliferation with an IC50 of
1.6 μM. The molecular mechanism study indicates that 6a significantly suppresses the oncogenic Erk kinase phosphorylation
at 3 μM.
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