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Title: Discovery of benzimidazole derivatives as novel multi-target EGFR, VEGFR-2 and PDGFR kinase inhibitors
Authors: Li, Y.
Tan, C.
Gao, C.
Zhang, C.
Luan, X.
Chen, X.
Liu, H.
Chen, Y. 
Jiang, Y.
Keywords: 2-Aryl benzimidazole
EGFR inhibitor
PDGFR inhibitor
VEGFR-2 inhibitor
Issue Date: 1-Aug-2011
Citation: Li, Y., Tan, C., Gao, C., Zhang, C., Luan, X., Chen, X., Liu, H., Chen, Y., Jiang, Y. (2011-08-01). Discovery of benzimidazole derivatives as novel multi-target EGFR, VEGFR-2 and PDGFR kinase inhibitors. Bioorganic and Medicinal Chemistry 19 (15) : 4529-4535. ScholarBank@NUS Repository.
Abstract: Multi-target EGFR, VEGFR-2 and PDGFR inhibitors are highly useful anticancer agents with improved therapeutic efficacies. In this work, we used two virtual screening methods, support vector machines (SVM) and molecular docking, to identify a novel series of benzimidazole derivatives, 2-aryl benzimidazole compounds, as multi-target EGFR, VEGFR-2 and PDGFR inhibitors. 2-Aryl benzimidazole compounds were synthesized and their biological activities against a tumor cell line HepG-2 and specific kinases were evaluated. Among these compounds, compounds 5a and 5e exhibited high cytotoxicity against HepG-2 cells with IC50 values at ∼2 μM. Further kinase assay study showed that compound 5a have good EGFR inhibitory activity and moderate VEGFR-2 and PDGFR inhibitory activities, while 5e have moderate EGFR inhibitory activity and slightly weaker VEGFR-2 and PDGFR inhibitory activities. Molecular docking analysis suggested that compound 5a more tightly interacts with EGFR and PDGFR than compound 5e. Our study discovered a novel series of benzimidazole derivatives as multi-target EGFR, VEGFR-2 and PDGFR kinases inhibitors. © 2011 Elsevier Ltd. All rights reserved.
Source Title: Bioorganic and Medicinal Chemistry
ISSN: 09680896
DOI: 10.1016/j.bmc.2011.06.022
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