Diversity-Oriented Synthesis of Imidazo-Dipyridines with Anticancer Activity via the Groebke–Blackburn–Bienaymé and TBAB-Mediated Cascade Reaction in One Pot
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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.
创建时间：
2019-07-30
