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Convenient synthetic method for 3-(3-substituted indol-2-yl)quinoxalin-2- ones as VEGF inhibitor
- フォーマット:
- 論文
- 責任表示:
- Aoki, Katsuyuki ; Koseki, Jun-ichi ; Takeda, Shuichi ; Aburada, Masaki ; Miyamoto, Kenichi
- 言語:
- 英語
- 出版情報:
- 日本薬学会, 2007-06-01
- 著者名:
- 掲載情報:
- Chemical and Pharmaceutical Bulletin
- ISSN:
- 0009-2363
- 巻:
- 55
- 通号:
- 6
- 開始ページ:
- 922
- 終了ページ:
- 925
- バージョン:
- publisher
- 概要:
- 金沢大学医学部附属病院薬剤部<br />It has already been reported that 3-(indol-2-yl)quinoxalin-2-ones 1)? have a potent inhibitory effect on the growth of tumor cells based on anti-angiogenesis activity. We have also carried out a structure-activity … relationship (SAR) study of 3-(indol-2-yl)quinoxalin-2-ones, which showed a potent inhibitory activity toward the vascular endothelial growth factor (VEGF)-induced proliferation of human mesangial cells and the VEGF-induced auto-phosphorylation of human umbilical vein endothelial cells.2) Moreover, one of these compounds has a potent medicinal effect based on anti-angiogenic action, by oral administration2) (Chart 1, 9). However, since the existing synthetic methods1) for the preparation of 3-(indol-2-yl)quinoxalin-2-ones consist of multiple steps some of which require strict anhydrous conditions, a convenient and simple synthetic method in place of the existing method is desirable. As a result of the investigations into the synthetic procedures, 3-(3-substituted indol-2-yl)quinoxalin-2-ones can be easily prepared by the condensation of 3-substituted indoles with quinoxalin-2-ones in the presence of trifluoroacetic acid (TFA). Herein, we report the examination of these reaction conditions and the application of this new synthetic method to the synthesis of the derivatives as VEGF inhibitors. © 2007 Pharmaceutical Society of Japan. 続きを見る
- URL:
- http://hdl.handle.net/2297/6594
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和漢医薬学会 = Medical and Pharmaceutical Society for WAKAN-YAKU | |
日本臨床薬理学会 = The Japanese Society of Clinical Pharmacology and Therapeutics | |
Pharmaceutical Society of Japan = 日本薬学会 | |
日本臨床薬理学会 = The Japanese Society of Clinical Pharmacology and Therapeutics |
Medical and Pharmaceutical Society for WAKAN-YAKU = 和漢医薬学会 |
Japan Institute of Heterocyclic Chemistry = 日本複素環化学研究所 |
日本複素環化学研究所 |