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


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.

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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.

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Correspondence to Hai-Tao Lan or Dong-Lin Yang or Cheng Yi.

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Zhang, M., Ding, Y., Qin, HX. et al. One-pot synthesis of substituted pyrrole–imidazole derivatives with anticancer activity. Mol Divers 24, 1177–1184 (2020).

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  • Pyrrole–imidazole
  • MCRs
  • Microwave irradiation
  • One pot
  • Anticancer activity