Diversity-Oriented Synthesis of Functionalized Imidazopyridine Analogues with Anti-Cancer Activity through a Transition-Metal Free, One-pot Cascade Reaction

Gui Ting Song, Nicholas McConnell, Zhong Zhu Chen, Xiao Fang Yao, Jiu Hong Huang, Jie Lei, Hui Kuan Lin, Brendan Frett, Hong Yu Li, Zhi Gang Xu

Research output: Contribution to journalArticlepeer-review

6 Scopus citations

Abstract

A transition-metal free, high yielding and efficient three-component reaction was designed and incorporated into two sequential oxidation and cyclization reaction cascades in one-pot with the assistance of microwave irradiation. A chemical collection of functionalized 3-substituted imidazopyridines was prepared by means of the mild reaction and simple operational procedure. The reaction has a broad tolerance for a variety of substituted carbonyl aldehydes, anilines and 2-phenyl-imidazo[1,2-a]pyridines. Screening in several cancer cell lines was conducted. Compound 9 i exhibited good potency against HeLa cell lines and this work validated the feasibility of the methodology for generating bioactive compounds.

Original languageEnglish (US)
JournalAdvanced Synthesis and Catalysis
DOIs
StateAccepted/In press - Jan 1 2018
Externally publishedYes

Keywords

  • Anti-cancer
  • Imidazopyridines
  • multicomponent reactions (MCRs)
  • One-pot
  • three-component reaction

ASJC Scopus subject areas

  • Catalysis
  • Organic Chemistry

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