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 journalArticle

27 Citations (Scopus)

Abstract

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
Volume20
Issue number12
DOIs
Publication statusPublished - 2010 May 10

Fingerprint

raf Kinases
Melanoma
Cells
Derivatives
Cell Line
Inhibitory Concentration 50
imidazole
Therapeutics

Keywords

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

ASJC Scopus subject areas

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

Cite this

1,4-Dihydropyrazolo[4,3-d]imidazole phenyl derivatives : A novel type II Raf kinase inhibitors. / Yu, Hana; Jung, Yunkyung; Kim, Hwan; Lee, Junghun; Oh, Chang Hyun; Yoo, Kyung Ho; Sim, Taebo; Hah, Jung Mi.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 20, No. 12, 10.05.2010, p. 3805-3808.

Research output: Contribution to journalArticle

Yu, Hana ; Jung, Yunkyung ; Kim, Hwan ; Lee, Junghun ; Oh, Chang Hyun ; Yoo, Kyung Ho ; Sim, Taebo ; Hah, Jung Mi. / 1,4-Dihydropyrazolo[4,3-d]imidazole phenyl derivatives : A novel type II Raf kinase inhibitors. In: Bioorganic and Medicinal Chemistry Letters. 2010 ; Vol. 20, No. 12. pp. 3805-3808.
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