Affordable Access

Publisher Website

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

Authors
Journal
Bioorganic & Medicinal Chemistry Letters
0960-894X
Publisher
Elsevier
Publication Date
Volume
20
Issue
5
Identifiers
DOI: 10.1016/j.bmcl.2010.01.064
Keywords
  • Pyrimidin-4-Yl-1H-Imidazol-2-Yl Derivatives
  • Antiproliferative Activity
  • Melanoma Cell Line
  • Braf
  • Craf
  • Selectivity

Abstract

Abstract The synthesis of a novel series of pyrimidin-4-yl-1 H-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 (IC 50 = 0.62 and 4.49 μM, respectively) and turned out to be a selective and potent CRAF inhibitor.

There are no comments yet on this publication. Be the first to share your thoughts.