Discovery and initial SAR of pyrimidin-4-yl-1H-imidazole derivatives with antiproliferative activity against melanoma cell lines

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

Research output: Contribution to journalArticlepeer-review

26 Citations (Scopus)

Abstract

The synthesis of a novel series of pyrimidin-4-yl-1H-imidazol-2-yl derivatives 7, 8, 9 and their antiproliferative activities against A375P human melanoma cell line and WM3629 cell line were described. Most compounds showed superior antiproliferative activities compared to Sorafenib, the well-known RAF inhibitor. Among them, 7a exhibited potent activities on both cell lines (IC50 = 0.62 and 4.49 μM, respectively) and turned out to be a selective and potent CRAF inhibitor.

Original languageEnglish
Pages (from-to)1573-1577
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume20
Issue number5
DOIs
Publication statusPublished - 2010 Mar 1

Keywords

  • Antiproliferative activity
  • BRAF
  • CRAF
  • Melanoma cell line
  • Pyrimidin-4-yl-1H-imidazol-2-yl derivatives
  • Selectivity

ASJC Scopus subject areas

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

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