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

被引:21
|
作者
Zhang, Ming [1 ,2 ,3 ]
Ding, Yong [4 ]
Qin, Hong-Xia [4 ]
Xu, Zhi-Gang [4 ]
Lan, Hai-Tao [2 ,3 ]
Yang, Dong-Lin [4 ]
Yi, Cheng [1 ]
机构
[1] Sichuan Univ, West China Hosp, Dept Abdominal Canc, West China Clin Med Sch, 37 Guoxue Xiang, Chengdu 610041, Peoples R China
[2] Univ Elect Sci & Technol China, Acad Med Sci, Canc Ctr, Chengdu 610000, Sichuan, Peoples R China
[3] Univ Elect Sci & Technol China, Affiliated Hosp, Sichuan Prov Peoples Hosp, Chengdu 610000, Sichuan, Peoples R China
[4] Chongqing Univ Arts & Sci, Int Acad Targeted Therapeut & Innovat, 319 Honghe Ave, Chongqing 402160, Peoples R China
关键词
Pyrrole-imidazole; MCRs; Microwave irradiation; One pot; Anticancer activity; RELATIVE CONFIGURATION; INDOLE; CYCLIZATION;
D O I
10.1007/s11030-019-09982-z
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
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.
引用
收藏
页码:1177 / 1184
页数:8
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