Art

J-GLOBAL ID：201702270725622461   Reference number：17A1783191

Design, synthesis, and evaluation of A-ring-modified lamellarin N analogues as noncovalent inhibitors of the EGFR T790M/L858R mutant

EGFR T790M/L858R変異体の非共有結合性阻害剤としてのA環修飾ラメラリンN類似体の設計,合成および評価【Powered by NICT】

Author (10)： Fukuda Tsutomu (Division of Chemistry and Materials Science, Graduate School of Engineering, Nagasaki University, 1-14 Bunkyo-machi, Nagasaki 852-8521, Japan) ,  Umeki Teppei (Division of Chemistry and Materials Science, Graduate School of Engineering, Nagasaki University, 1-14 Bunkyo-machi, Nagasaki 852-8521, Japan) ,  Tokushima Keiji (Division of Chemistry and Materials Science, Graduate School of Engineering, Nagasaki University, 1-14 Bunkyo-machi, Nagasaki 852-8521, Japan) ,  Xiang Gao (Division of Chemistry and Materials Science, Graduate School of Engineering, Nagasaki University, 1-14 Bunkyo-machi, Nagasaki 852-8521, Japan) ,  Yoshida Yuki (Division of Chemistry and Materials Science, Graduate School of Engineering, Nagasaki University, 1-14 Bunkyo-machi, Nagasaki 852-8521, Japan) ,  Ishibashi Fumito (Division of Marine Life Science and Biochemistry, Graduate School of Fisheries and Environmental Sciences, Nagasaki University, 1-14 Bunkyo-machi, Nagasaki 852-8521, Japan) ,  Oku Yusuke (Department of Integrated Information for Pharmaceutical Sciences, Iwate Medical University School of Pharmacy, 2-1-1 Nishitokuta, Yahaba-cho, Shiwa-gun, Iwate 028-3694, Japan) ,  Nishiya Naoyuki (Department of Integrated Information for Pharmaceutical Sciences, Iwate Medical University School of Pharmacy, 2-1-1 Nishitokuta, Yahaba-cho, Shiwa-gun, Iwate 028-3694, Japan) ,  Uehara Yoshimasa (Department of Integrated Information for Pharmaceutical Sciences, Iwate Medical University School of Pharmacy, 2-1-1 Nishitokuta, Yahaba-cho, Shiwa-gun, Iwate 028-3694, Japan) ,  Iwao Masatomo (Division of Chemistry and Materials Science, Graduate School of Engineering, Nagasaki University, 1-14 Bunkyo-machi, Nagasaki 852-8521, Japan)
Material： Bioorganic & Medicinal Chemistry  (Bioorganic and Medicinal Chemistry)
Volume： 25  Issue： 24  Page： 6563-6580  Publication year： Dec. 15, 2017 
JST Material Number： W0556A  ISSN： 0968-0896  Document type： Article
Article type： 原著論文  Country of issue： Netherlands (NLD)  Language： ENGLISH (EN)

Abstract/Point： A series of A-ring-modified la...

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Thesaurus term： *EGF receptor ,  *mutant ,  drug resistance ,  non-small cell lung cancer ,  *enzyme inhibitor ,  docking ,  molecular recognition ,  drug design ,  solubility(property) ,  *nitrogen heterocyclic compound ,  *oxygen heterocyclic compound ,  binding site ,  *polynuclear aromatic compound ,  solubility
Semi thesaurus term： *EGFR-tyrosine kinase inhibitor ,  SBDD ,  *ラメラリンN誘導体 ,  molecular docking

Author keywords (5)： EGFR tyrosine kinase inhibitors (EGFR-TKI) ,  EGFR T790M/L858R mutant ,  Structure-based drug design (SBDD) ,  Lamellarin N ,  Water-soluble analogues

JST classification (8)： Oxygen heterocycles in general  (CF07020K) ,  Nitrogen heterocycles in general  (CF07040G) ,  Condensed tetra-or more-cyclic carbocyclic compounds  (CF06090C) ,  Basic oncology in general  (GE02010R) ,  Synthesis of drugs  (GV01030F) ,  Structure-activity relationship of drugs  (GV01050B) ,  Basic research of antitumor(=antineoplastic)drugs  (GW16010A) ,  Basic research of enzyme preparations and enzyme inhibitor preparations  (GW21010W)

Substance index (1)： Lamellarin 14

Terms in the title (9)： EGFR ,  変異体 ,  非共有結合 ,  阻害剤 ,  修飾 ,  ラメラリンN ,  類似体 ,  設計 ,  評価