Diversity-Oriented Synthesis of Imidazo-Dipyridines with Anticancer Activity via the Groebke-Blackburn-Bienaymé and TBAB-Mediated Cascade Reaction in One Pot

Yong Li, Jiu Hong Huang, Juan Li Wang, Gui Ting Song, Dian Yong Tang, Fang Yao, Hui Kuan Lin, Wei Yan, Hong Yu Li, Zhi Gang Xu, Zhong Zhu Chen

Research output: Contribution to journalArticle


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.

Original languageEnglish (US)
JournalJournal of Organic Chemistry
Publication statusAccepted/In press - Jan 1 2019


ASJC Scopus subject areas

  • Organic Chemistry

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