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 journalArticle

25 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

Fingerprint

Melanoma
Cells
Derivatives
Cell Line
Inhibitory Concentration 50
imidazole
sorafenib

Keywords

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

ASJC Scopus subject areas

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

Cite this

Discovery and initial SAR of pyrimidin-4-yl-1H-imidazole derivatives with antiproliferative activity against melanoma cell lines. / Lee, Junghun; Kim, Hwan; Yu, Hana; Chung, Jae Yoon; Oh, Chang Hyun; Yoo, Kyung Ho; Sim, Taebo; Hah, Jung Mi.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 20, No. 5, 01.03.2010, p. 1573-1577.

Research output: Contribution to journalArticle

Lee, Junghun ; Kim, Hwan ; Yu, Hana ; Chung, Jae Yoon ; Oh, Chang Hyun ; Yoo, Kyung Ho ; Sim, Taebo ; Hah, Jung Mi. / Discovery and initial SAR of pyrimidin-4-yl-1H-imidazole derivatives with antiproliferative activity against melanoma cell lines. In: Bioorganic and Medicinal Chemistry Letters. 2010 ; Vol. 20, No. 5. pp. 1573-1577.
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