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通过三组分级联缩合合成具有抗癌活性的吡啶并二吲哚。

Synthesis of Pyridodiindoles with Anticancer Activity by a Three-Component Cascade Condensation.

机构信息

Chongqing Engineering Laboratory of Targeted and Innovative Therapeutics, Chongqing Key Laboratory of Kinase Modulators as Innovative Medicine, IATTI , Chongqing University of Arts and Sciences . 319 Honghe Avenue , Yongchuan , Chongqing 402160 , China.

Department of Pharmaceutical Sciences, College of Pharmacy , University of Arkansas for Medical Sciences , Little Rock , Arkansas 72205 , United States.

出版信息

Org Lett. 2018 Dec 21;20(24):7811-7815. doi: 10.1021/acs.orglett.8b03245. Epub 2018 Dec 4.

Abstract

A novel three-component cascade reaction was discovered and developed to synthesize pyridodiindoles with the assistance of microwave irradiation. A collection of pyridodiindoles was prepared by means of the mild reaction and simple operation procedure, which could be applicable to a broad scope of functional aldehydes. Screening demonstrated that compound 5g exhibited a good potency in HCT116 cell lines, and this work validated the feasibility of this novel reaction for generating promising bioactive compounds.

摘要

一种新型的三组分级联反应在微波辐射的辅助下被发现并发展用于合成吡啶并二吲哚。通过温和的反应和简单的操作程序制备了一系列吡啶并二吲哚,该方法适用于广泛的功能醛。筛选表明,化合物 5g 在 HCT116 细胞系中表现出良好的活性,这项工作验证了这种新型反应生成有前途的生物活性化合物的可行性。

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