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

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Title
Discovery of fluorescent 3-heteroarylcoumarin derivatives as novel inhibitors of anaplastic lymphoma kinase
Author(s)
Shinmee Mah; Jaebong Jang; Daesun Song; Yongje Shin; Muhammad Latif; Yongwon Jung; Sungwoo Hong
Publication Date
2019-01
Journal
ORGANIC & BIOMOLECULAR CHEMISTRY, v.17, no.1, pp.186 - 194
Publisher
ROYAL SOC CHEMISTRY
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 © The Royal Society of Chemistry 2019
URI
https://pr.ibs.re.kr/handle/8788114/5602
ISSN
1477-0520
Appears in Collections:
Center for Catalytic Hydrocarbon Functionalizations(분자활성 촉매반응 연구단) > Journal Papers (저널논문)
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