Please use this identifier to cite or link to this item:
https://doi.org/10.1016/j.bmc.2011.06.022
DC Field | Value | |
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dc.title | Discovery of benzimidazole derivatives as novel multi-target EGFR, VEGFR-2 and PDGFR kinase inhibitors | |
dc.contributor.author | Li, Y. | |
dc.contributor.author | Tan, C. | |
dc.contributor.author | Gao, C. | |
dc.contributor.author | Zhang, C. | |
dc.contributor.author | Luan, X. | |
dc.contributor.author | Chen, X. | |
dc.contributor.author | Liu, H. | |
dc.contributor.author | Chen, Y. | |
dc.contributor.author | Jiang, Y. | |
dc.date.accessioned | 2014-10-29T01:51:27Z | |
dc.date.available | 2014-10-29T01:51:27Z | |
dc.date.issued | 2011-08-01 | |
dc.identifier.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. https://doi.org/10.1016/j.bmc.2011.06.022 | |
dc.identifier.issn | 09680896 | |
dc.identifier.uri | http://scholarbank.nus.edu.sg/handle/10635/105839 | |
dc.description.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. | |
dc.description.uri | http://libproxy1.nus.edu.sg/login?url=http://dx.doi.org/10.1016/j.bmc.2011.06.022 | |
dc.source | Scopus | |
dc.subject | 2-Aryl benzimidazole | |
dc.subject | Anticancer | |
dc.subject | EGFR inhibitor | |
dc.subject | Multi-target | |
dc.subject | PDGFR inhibitor | |
dc.subject | VEGFR-2 inhibitor | |
dc.type | Article | |
dc.contributor.department | PHARMACY | |
dc.description.doi | 10.1016/j.bmc.2011.06.022 | |
dc.description.sourcetitle | Bioorganic and Medicinal Chemistry | |
dc.description.volume | 19 | |
dc.description.issue | 15 | |
dc.description.page | 4529-4535 | |
dc.description.coden | BMECE | |
dc.identifier.isiut | 000292913400013 | |
Appears in Collections: | Staff Publications |
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