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Diversity‐Oriented Synthesis of Functionalized Imidazopyridine Analogues with Anti‐Cancer Activity through a Transition‐Metal Free, One‐pot Cascade Reaction
Author(s) -
Song GuiTing,
McConnell Nicholas,
Chen ZhongZhu,
Yao XiaoFang,
Huang JiuHong,
Lei Jie,
Lin HuiKuan,
Frett Brendan,
Li Hongyu,
Xu ZhiGang
Publication year - 2018
Publication title -
advanced synthesis and catalysis
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.541
H-Index - 155
eISSN - 1615-4169
pISSN - 1615-4150
DOI - 10.1002/adsc.201800728
Subject(s) - chemistry , imidazopyridine , combinatorial chemistry , cascade reaction , transition metal , hela , microwave irradiation , reaction conditions , organic chemistry , catalysis , in vitro , biochemistry
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.