Discovery of fluorescent 3-heteroarylcoumarin derivatives as novel inhibitors of anaplastic lymphoma kinase

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dc.contributor.authorMah, Shinmeeko
dc.contributor.authorJang, Jaebongko
dc.contributor.authorSong, Daesunko
dc.contributor.authorShin, Yongjeko
dc.contributor.authorLatif, Muhammadko
dc.contributor.authorJung, Yongwonko
dc.contributor.authorHong, Sungwooko
dc.date.accessioned2019-01-23T06:54:52Z-
dc.date.available2019-01-23T06:54:52Z-
dc.date.created2019-01-14-
dc.date.issued2019-01-
dc.identifier.citationORGANIC BIOMOLECULAR CHEMISTRY, v.17, no.1, pp.186 - 194-
dc.identifier.issn1477-0520-
dc.identifier.urihttp://hdl.handle.net/10203/250118-
dc.description.abstractAltered expression or hyperactivation of anaplastic lymphoma kinase (ALK), as a consequence of translocations or point mutations, is one of the main oncogenic drivers in non-small cell lung cancer. Using structure-based design and in vitro enzyme assays, we identified 3-heteroarylcoumarin as a new template for the development of novel fluorescent ALK inhibitors. Molecular simulation provided structural insights for the design of 3-heteroarylcoumarin derivatives, which were easily prepared through efficient synthetic approaches including direct C-H cross coupling. Importantly, these coumarin-based ALK inhibitors can be tracked using microscopy techniques: we illustrated the use of the most potent compound in this series, 5a, (ALK/IC50 = 0.51 M, (emi) = 500 nm, phi(F) = 0.29) to monitor its subcellular distribution pattern by confocal fluorescence microscopy.-
dc.languageEnglish-
dc.publisherROYAL SOC CHEMISTRY-
dc.titleDiscovery of fluorescent 3-heteroarylcoumarin derivatives as novel inhibitors of anaplastic lymphoma kinase-
dc.typeArticle-
dc.identifier.wosid000454251100022-
dc.identifier.scopusid2-s2.0-85058839879-
dc.type.rimsART-
dc.citation.volume17-
dc.citation.issue1-
dc.citation.beginningpage186-
dc.citation.endingpage194-
dc.citation.publicationnameORGANIC BIOMOLECULAR CHEMISTRY-
dc.identifier.doi10.1039/c8ob02874e-
dc.contributor.localauthorJung, Yongwon-
dc.contributor.localauthorHong, Sungwoo-
dc.contributor.nonIdAuthorJang, Jaebong-
dc.contributor.nonIdAuthorLatif, Muhammad-
dc.description.isOpenAccessN-
dc.type.journalArticleArticle-
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