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

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Diversity‐Oriented Synthesis of Functionalized Imidazopyridine Analogues with Anti‐Cancer Activity through a Transition‐Metal Free, One‐pot Cascade Reaction
Advanced Synthesis & Catalysis ( IF 4.4 ) Pub Date : 2018-08-09 , DOI: 10.1002/adsc.201800728
Gui-Ting Song ₁ , Nicholas McConnell _{2,

3} , Zhong-Zhu Chen ₁ , Xiao-Fang Yao ₁ , Jiu-Hong Huang ₁ , Jie Lei ₁ , Hui-Kuan Lin ₄ , Brendan Frett ₂ , Hong-yu Li ₂ , Zhi-Gang Xu ₁

Affiliation

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.

中文翻译：

通过无过渡金属的单锅级联反应，具有抗癌活性的功能化咪唑并吡啶类似物的多样性导向合成

设计了无过渡金属，高产率和高效的三组分反应，并借助微波辐射将其整合到一个锅中的两个顺序的氧化和环化反应级联中。通过温和的反应和简单的操作步骤，制备了功能化的3-取代的咪唑并吡啶的化学物质。该反应对各种取代的羰基醛，苯胺和2-苯基-咪唑并[1,2- a ]吡啶具有宽泛的耐受性。进行了几种癌细胞系的筛选。化合物9 i对HeLa细胞系表现出良好的效力，这项工作证实了产生生物活性化合物的方法的可行性。

更新日期：2018-08-09

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