Please use this identifier to cite or link to this item: https://doi.org/10.1016/j.bmc.2011.06.022
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dc.titleDiscovery of benzimidazole derivatives as novel multi-target EGFR, VEGFR-2 and PDGFR kinase inhibitors
dc.contributor.authorLi, Y.
dc.contributor.authorTan, C.
dc.contributor.authorGao, C.
dc.contributor.authorZhang, C.
dc.contributor.authorLuan, X.
dc.contributor.authorChen, X.
dc.contributor.authorLiu, H.
dc.contributor.authorChen, Y.
dc.contributor.authorJiang, Y.
dc.date.accessioned2014-10-29T01:51:27Z
dc.date.available2014-10-29T01:51:27Z
dc.date.issued2011-08-01
dc.identifier.citationLi, 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. https://doi.org/10.1016/j.bmc.2011.06.022
dc.identifier.issn09680896
dc.identifier.urihttp://scholarbank.nus.edu.sg/handle/10635/105839
dc.description.abstractMulti-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.
dc.description.urihttp://libproxy1.nus.edu.sg/login?url=http://dx.doi.org/10.1016/j.bmc.2011.06.022
dc.sourceScopus
dc.subject2-Aryl benzimidazole
dc.subjectAnticancer
dc.subjectEGFR inhibitor
dc.subjectMulti-target
dc.subjectPDGFR inhibitor
dc.subjectVEGFR-2 inhibitor
dc.typeArticle
dc.contributor.departmentPHARMACY
dc.description.doi10.1016/j.bmc.2011.06.022
dc.description.sourcetitleBioorganic and Medicinal Chemistry
dc.description.volume19
dc.description.issue15
dc.description.page4529-4535
dc.description.codenBMECE
dc.identifier.isiut000292913400013
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