Antitumor studies. Part 1: Design, synthesis, antitumor activity, and AutoDock study of 2-deoxo-2-phenyl-5-deazaflavins and 2-deoxo-2-phenylflavin-5-oxides as a new class of antitumor agents

Ali, Hamed I..; Tomita, Keiichiro; Akaho, Eiichi; Kambara, Hiroto; Miura, Shinji; Hayakawa, Hiroyuki; Ashida, Noriyuki; Kawashima, Yutaka; Yamagishi, Takehiro; Ikeya, Hisao; Yoneda, Fumio; Nagamatsu, Tomohisa

doi:10.1016/j.bmc.2006.09.063

Permalink : https://ousar.lib.okayama-u.ac.jp/34207

ID	34207
フルテキストURL	fulltext.pdf 2.6 MB
著者	Ali, Hamed I.. Division of Pharmaceutical Sciences, Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, Okayama University Tomita, Keiichiro Division of Pharmaceutical Sciences, Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, Okayama University Akaho, Eiichi Faculty of Pharmaceutical Sciences, High Technology Research Center (Life Science Center), and Center for Area Research and Development, Kobe Gakuin University Kambara, Hiroto Faculty of Pharmaceutical Sciences, High Technology Research Center (Life Science Center), and Center for Area Research and Development, Kobe Gakuin University Miura, Shinji Biology Laboratory, Research and Development Division, Yamasa Shoyu Co. Hayakawa, Hiroyuki Biology Laboratory, Research and Development Division, Yamasa Shoyu Co. Ashida, Noriyuki Biology Laboratory, Research and Development Division, Yamasa Shoyu Co. Kawashima, Yutaka Medicinal Research Laboratories, Taisho Pharmaceutical Co. Yamagishi, Takehiro Medicinal Research Laboratories, Taisho Pharmaceutical Co. Ikeya, Hisao Medicinal Research Laboratories, Taisho Pharmaceutical Co. Yoneda, Fumio Faculty of Pharmaceutical Sciences, Kyoto University Nagamatsu, Tomohisa Division of Pharmaceutical Sciences, Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, Okayama University Kaken ID publons researchmap
抄録	Novel 2-deoxo-2-phenyl-5-deazaflavins and 2-deoxo-2-phenylflavin-5-oxides were prepared as a new class of antitumor agents and showed significant antitumor activities against NCI-H 460, HCT 116, A 431, CCRF-HSB-2, and KB cell lines. In vivo investigation, 2-deoxo-10-methyl-2-phenyl-5-deazaflavin exhibited the effective antitumor activity against A 431 human adenocarcinoma cells transplanted subcutaneously into nude mouse. Furthermore, AutoDock study has been done by binding of the flavin analogs into PTK pp60(c-src), where a good correlation between their IC50 and AutoDock binding free energy was exhibited. In particular, 2-deoxo-2-phenylflavin-5-oxides exhibited the highest potential binding affinity within the binding pocket of PTK.
キーワード	antitumor activity Flavin analog 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.1 pp.242-256 Publisher URL: http://dx.doi.org/10.1016/j.bmc.2006.09.063 Direct access to Thomson Web of Science record Copyright © 2007 by Elsevier Ltd.
発行日	2007-01-01
出版物タイトル	Bioorganic & Medicinal Chemistry
巻	15巻
号	1号
出版者	Pergamon-Elsevier Science Ltd.
開始ページ	242
終了ページ	256
ISSN	0968-0896
NCID	AA10938083
資料タイプ	学術雑誌論文
言語	英語
著作権者	Elsevier Ltd.
論文のバージョン	author
査読	有り
DOI	10.1016/j.bmc.2006.09.063
PubMed ID	17049252
Web of Science KeyUT	000243087200022
Submission Path	organic_chemistry/11