| ID | 34203 |
| フルテキストURL | |
| 著者 |
Ali, Hamed I.
Department of Drug Discovery and Development, Division of Pharmaceutical Sciences, Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, Okayama University
Ashida, Noriyuki
Biology Laboratory, Research and Development Division, Yamasa Shoyu Co.
Nagamatsu, Tomohisa
aDepartment of Drug Discovery and Development, Division of Pharmaceutical Sciences, Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, Okayama University
Kaken ID
publons
researchmap
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| 抄録 | Various novel 10-alkyl-2-deoxo-2-methylthio-5-deazaflavins have been synthesized by reaction of 6-(N-alkylanilino)-2-methylthiopyrimidin-4(3H)-ones with Vilsmeier reagent. The similar 2-(N-substituted amino) derivatives were prepared by nucleophilic replacement reaction of the 2-methylthio moiety by appropriate amines. The 2-oxo derivatives (i.e., 5-deazaflavins) were obtained by acidic hydrolysis of the 2-methylthio derivatives. The antitumor activities against CCRF-HSB-2 and KB cells and the antiviral activities against HSV-1 and HSV-2 have been investigated in vitro, and many compounds showed promising antitumor activities. Furthermore, AutoDock molecular docking into PTK has been done for lead optimization of these compounds as potential PTK inhibitors. Whereas, the designed 2-deoxo-5-deazaflavins connected with amino acids at the 2-position exhibited the good binding affinities into PTK with more hydrogen bonds.
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| キーワード | antitumor activity
5-deazaflavin
AutoDock
protein tyrosine
kinase
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| 備考 | Published with permission from the copyright holder.
This is a author's copy,as published in Bioorganic & Medicinal Chemistry , 2007 Vol.15 Issue.19 pp.6336-6352 Publisher URL: http://dx.doi.org/10.1016/j.bmc.2007.06.058 Direct access to Thomson Web of Science record Copyright © 2008 by Elsevier Ltd. |
| 発行日 | 2007-10-01
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| 出版物タイトル |
Bioorganic & Medicinal Chemistry
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| 巻 | 15巻
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| 号 | 19号
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| 出版者 | Pergamon-Elsevier Science Ltd.
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| 開始ページ | 6336
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| 終了ページ | 6352
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| ISSN | 0968-0896
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| NCID | AA10938083
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| 資料タイプ |
学術雑誌論文
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| 言語 |
英語
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| 著作権者 | Elsevier Ltd.
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| 論文のバージョン | author
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| 査読 |
有り
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| DOI | |
| PubMed ID | |
| Web of Science KeyUT | |
| Submission Path | organic_chemistry/12
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