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

  • Ming Zhang
  • Yong Ding
  • Hong-Xia Qin
  • Zhi-Gang Xu
  • Hai-Tao LanEmail author
  • Dong-Lin YangEmail author
  • Cheng YiEmail author
Original Article


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.

Graphic abstract


Pyrrole–imidazole MCRs Microwave irradiation One pot Anticancer activity 



The authors would like to thank the Sichuan Provincial Science and Technology (2017fz0084), the Sichuan Province medical association (s15074), Chongqing Research Program of Basic Research and Frontier Technology (cstc2016jcyjA0534 and cstc2018jcyjAX0219) and the Scientific Research Foundation of the Chongqing University of Arts and Sciences (R2013XY01, R2015BX03, 2017ZBX05 and 2017ZBX10). We would also like to thank Ms H.Z. Liu for obtaining the LC/MS and NMR data.

Compliance with ethical standards

Conflict of interest

The authors have declared no conflict of interest.

Supplementary material

11030_2019_9982_MOESM1_ESM.pdf (1.8 mb)
Supplementary material 1 (PDF 1844 kb)


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Copyright information

© Springer Nature Switzerland AG 2019

Authors and Affiliations

  1. 1.Department of Abdominal Cancer, West China Hospital, West China Clinical Medical SchoolSichuan UniversityChengduChina
  2. 2.Cancer Center, Academy of Medical Sciences and Sichuan Provincial People’s HospitalAffiliated Hospital of University of Electronic Science and Technology of ChinaChengduChina
  3. 3.International Academy of Targeted Therapeutics and InnovationChongqing University of Arts and SciencesChongqingChina

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