1,4-Dihydropyrazolo[4,3-d]imidazole phenyl derivatives: A novel type II Raf kinase inhibitors

Hana Yu, Yunkyung Jung, Hwan Kim, Junghun Lee, Chang Hyun Oh, Kyung Ho Yoo, Taebo Sim, Jung Mi Hah

Research output: Contribution to journalArticlepeer-review

33 Citations (Scopus)


The synthesis of a novel series of 1,4-dihydropyrazolo[4,3-d]imidazole phenyl derivatives 1a-b, 2a-v and their antiproliferative activities against A375P and WM3629 human melanoma cell line were described. Most compounds showed competitive antiproliferative activities to sorafenib, the reference standard. Among them, pyrazoloimidazole phenyl urea compounds 2a, 2d, 2g, 2i, 2t exhibited potent activities on WM3629 cell lines (IC50 = 0.56-0.86 μM). Especially, 2t was found to be a potent and selective C-Raf inhibitor, showing a possibility as melanoma therapeutics.

Original languageEnglish
Pages (from-to)3805-3808
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Issue number12
Publication statusPublished - 2010

Bibliographical note

Funding Information:
This research was supported by Korea Institute of Science and Technology and Basic Science Research Program through the National Research Foundation of Korea (NRF) funded by the Ministry of Education, Science and Technology ( 2009-0087992 ; J.M.H.).


  • 1,4-Dihydropyrazolo[4,3-d]imidazole phenyl derivatives
  • Antiproliferative activity
  • Melanoma cell line
  • Selectivity

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry


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