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ID 34203
フルテキストURL
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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
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.
キーワード
antitumor activity
5-deazaflavin
AutoDock
protein tyrosine
kinase
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
出版物タイトル
Bioorganic & Medicinal Chemistry
15巻
19号
出版者
Pergamon-Elsevier Science Ltd.
開始ページ
6336
終了ページ
6352
ISSN
0968-0896
NCID
AA10938083
資料タイプ
学術雑誌論文
言語
English
著作権者
Elsevier Ltd.
論文のバージョン
author
査読
有り
DOI
PubMed ID
Web of Sience KeyUT
Submission Path
organic_chemistry/12