DC Field | Value | Language |
---|---|---|
dc.contributor.author | Mah, Shinmee | ko |
dc.contributor.author | Jang, Jaebong | ko |
dc.contributor.author | Song, Daesun | ko |
dc.contributor.author | Shin, Yongje | ko |
dc.contributor.author | Latif, Muhammad | ko |
dc.contributor.author | Jung, Yongwon | ko |
dc.contributor.author | Hong, Sungwoo | ko |
dc.date.accessioned | 2019-01-23T06:54:52Z | - |
dc.date.available | 2019-01-23T06:54:52Z | - |
dc.date.created | 2019-01-14 | - |
dc.date.issued | 2019-01 | - |
dc.identifier.citation | ORGANIC BIOMOLECULAR CHEMISTRY, v.17, no.1, pp.186 - 194 | - |
dc.identifier.issn | 1477-0520 | - |
dc.identifier.uri | http://hdl.handle.net/10203/250118 | - |
dc.description.abstract | Altered 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.language | English | - |
dc.publisher | ROYAL SOC CHEMISTRY | - |
dc.title | Discovery of fluorescent 3-heteroarylcoumarin derivatives as novel inhibitors of anaplastic lymphoma kinase | - |
dc.type | Article | - |
dc.identifier.wosid | 000454251100022 | - |
dc.identifier.scopusid | 2-s2.0-85058839879 | - |
dc.type.rims | ART | - |
dc.citation.volume | 17 | - |
dc.citation.issue | 1 | - |
dc.citation.beginningpage | 186 | - |
dc.citation.endingpage | 194 | - |
dc.citation.publicationname | ORGANIC BIOMOLECULAR CHEMISTRY | - |
dc.identifier.doi | 10.1039/c8ob02874e | - |
dc.contributor.localauthor | Jung, Yongwon | - |
dc.contributor.localauthor | Hong, Sungwoo | - |
dc.contributor.nonIdAuthor | Jang, Jaebong | - |
dc.contributor.nonIdAuthor | Latif, Muhammad | - |
dc.description.isOpenAccess | N | - |
dc.type.journalArticle | Article | - |
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