Please use this identifier to cite or link to this item: https://doi.org/10.1016/j.bmc.2012.04.006
Title: Exploration of 1-(3-chloro-4-(4-oxo-4H-chromen-2-yl)phenyl)-3-phenylurea derivatives as selective dual inhibitors of Raf1 and JNK1 kinases for anti-tumor treatment
Authors: Jin, F.
Gao, D.
Zhang, C.
Liu, F.
Chu, B.
Chen, Y.
Chen, Y.Z. 
Tan, C.
Jiang, Y.
Keywords: Aromatic urea
Flavones
Hepatocellular carcinoma
JNK
Kinases inhibitors
Raf
Issue Date: 1-Feb-2013
Citation: Jin, F., Gao, D., Zhang, C., Liu, F., Chu, B., Chen, Y., Chen, Y.Z., Tan, C., Jiang, Y. (2013-02-01). Exploration of 1-(3-chloro-4-(4-oxo-4H-chromen-2-yl)phenyl)-3-phenylurea derivatives as selective dual inhibitors of Raf1 and JNK1 kinases for anti-tumor treatment. Bioorganic and Medicinal Chemistry 21 (3) : 824-831. ScholarBank@NUS Repository. https://doi.org/10.1016/j.bmc.2012.04.006
Abstract: Based on the roles of Raf1 and JNK1 in hepatocarcinoma development, scaffold-based drug design was employed to produce a series of compounds, which subsequently were synthesized and explored as potential dual inhibitors Raf1 and JNK1 kinases for anti-tumor treatment. The compound 1-(3-chloro-4-(6-ethyl-4- oxo-4H-chromen-2-yl)phenyl)-3-(4-chloro-phenyl)urea (3d) showed 66%, 67% and 13% inhibition rate at 50 μM against Raf1, JNK1 and p38-alpha, respectively, but no effect on ERK1 and ERK2, and inhibited the expression of pERK1/2 markedly and HepG2 cells proliferation with IC50 at 8.3 μM. Furthermore, 3d showed lower toxicity against normal liver cell-lines QSG7701 and HL7702. Molecular docking study further showed that 3d can fit into binding domain of JNK1 and Raf1. Our data suggested the activities of 3d were associated with dual inhibition of JNK1 and Raf1 kinases. © 2012 Elsevier Ltd. All rights reserved.
Source Title: Bioorganic and Medicinal Chemistry
URI: http://scholarbank.nus.edu.sg/handle/10635/105943
ISSN: 09680896
DOI: 10.1016/j.bmc.2012.04.006
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