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一锅法合成具有抗癌活性的取代吡咯并咪唑衍生物。

One-pot synthesis of substituted pyrrole-imidazole derivatives with anticancer activity.

机构信息

Department of Abdominal Cancer, West China Hospital, West China Clinical Medical School, Sichuan University, 37 Guoxue Xiang, Chengdu, 610041, China.

Cancer Center, Academy of Medical Sciences and Sichuan Provincial People's Hospital, Affiliated Hospital of University of Electronic Science and Technology of China, Chengdu, 610000, Sichuan, China.

出版信息

Mol Divers. 2020 Nov;24(4):1177-1184. doi: 10.1007/s11030-019-09982-z. Epub 2019 Sep 7.

Abstract

A facile and efficient method to synthesize pyrrole-imidazole was developed via a post-Ugi cascade reaction followed by one purification procedure. Synthesized pyrrole-imidazole was collected by performing a mild reaction and a simple procedure, which could be applicable to a broad scope of functionalized anilines. The screening results demonstrated that compound 7e exhibited a high potency of anticancer activity in human pancreatic cancer cell lines PANC and ASPC-1. Our work shed light on the potential of post-Ugi cascade reaction in combinatorial and medicinal chemistry.

摘要

我们开发了一种简便高效的吡咯并咪唑合成方法,通过 Ugi 后级联反应和一步纯化步骤即可实现。通过温和的反应和简单的步骤收集合成的吡咯并咪唑,可以适用于广泛的功能化苯胺。筛选结果表明,化合物 7e 在人胰腺癌细胞系 PANC 和 ASPC-1 中表现出很强的抗癌活性。我们的工作为 Ugi 后级联反应在组合化学和药物化学中的应用提供了新的思路。

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