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Design, synthesis and biological evaluation of benzyl 2-(1H-imidazole-1-yl) pyrimidine analogues as selective and potent Raf inhibitors
- Authors
- Kim, Minjung; Lee, Junghun; Jung, Kyungjin; Kim, Hyangmi; Aman, Wagar; Ryu, Jae-Sang; Hah, Jung-Mi
- Issue Date
- Aug-2014
- Publisher
- PERGAMON-ELSEVIER SCIENCE LTD
- Keywords
- (4-Aminobenzyl)-1H-imidazol-1-yl pyrimidin-2-yl derivatives; Antiproliferative activity; Melanoma; BRAF V600E; CRAF; Selectivity
- Citation
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.24, no.15, pp.3600 - 3604
- Indexed
- SCIE
SCOPUS
- Journal Title
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- Volume
- 24
- Number
- 15
- Start Page
- 3600
- End Page
- 3604
- ISSN
- 0960-894X
- 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 91, 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). (C) 2014 Elsevier Ltd. All rights reserved.
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Related Researcher
- Hah, Jung Mi
- COLLEGE OF PHARMACY (DEPARTMENT OF PHARMACY)