Design, synthesis and biological evaluation of benzyl 2-(1H-imidazole-1-yl) pyrimidine analogues as selective and potent Raf inhibitors

Minjung Kim, Junghun Lee, Kyungjin Jung, Hyangmi Kim, Waqar Aman, Jae Sang Ryu, Jung Mi Hah

Research output: Contribution to journalArticlepeer-review

14 Scopus citations

Abstract

The synthesis of a novel series of (4-aminobenzyl/benzoyl)-1H-imidazol-1-yl pyrimidin-2-yl derivatives 9, 10, 18, 19 and their in vitro antiproliferative activities against the A375P human melanoma cell line and the U937 human leukemic monocyte lymphoma cell line are described. Potent antiproliferative effects were found from 9l, 9s and 10c; 10c was found to be a highly potent and selective BRAF V600E and CRAF inhibitor (IC50 = 38.3 nM and 8.79 nM).

Original languageEnglish
Pages (from-to)3600-3604
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume24
Issue number15
DOIs
StatePublished - 1 Aug 2014

Keywords

  • (4-Aminobenzyl)-1H-imidazol-1-yl pyrimidin-2-yl derivatives
  • Antiproliferative activity
  • BRAF V600E
  • CRAF
  • Melanoma
  • Selectivity

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