WEKO3
インデックスリンク
アイテム
Convenient synthetic method for 3-(3-substituted indol-2-yl)quinoxalin-2- ones as VEGF inhibitor
http://hdl.handle.net/2297/6594
http://hdl.handle.net/2297/6594f55941ae-336a-4783-bc15-27a074f72224
| 名前 / ファイル | ライセンス | アクション |
|---|---|---|
HO-PR-MIYAMOTO-K-922.pdf (137.7 kB)
|
|
| Item type | 学術雑誌論文 / Journal Article(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2017-10-05 | |||||
| タイトル | ||||||
| タイトル | Convenient synthetic method for 3-(3-substituted indol-2-yl)quinoxalin-2- ones as VEGF inhibitor | |||||
| 言語 | ||||||
| 言語 | eng | |||||
| 資源タイプ | ||||||
| 資源タイプ識別子 | http://purl.org/coar/resource_type/c_6501 | |||||
| 資源タイプ | journal article | |||||
| 著者 |
Aoki, Katsuyuki
× Aoki, Katsuyuki× Koseki, Jun-ichi× Takeda, Shuichi× Aburada, Masaki× Miyamoto, Kenichi |
|||||
| 提供者所属 | ||||||
| 内容記述タイプ | Other | |||||
| 内容記述 | 金沢大学医学部附属病院薬剤部 | |||||
| 書誌情報 |
Chemical and Pharmaceutical Bulletin 巻 55, 号 6, p. 922-925, 発行日 2007-06-01 |
|||||
| ISSN | ||||||
| 収録物識別子タイプ | ISSN | |||||
| 収録物識別子 | 0009-2363 | |||||
| DOI | ||||||
| 関連タイプ | isIdenticalTo | |||||
| 識別子タイプ | DOI | |||||
| 関連識別子 | https://doi.org/10.1248/cpb.55.922 | |||||
| 出版者 | ||||||
| 出版者 | 日本薬学会 | |||||
| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | 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. | |||||
| 著者版フラグ | ||||||
| 出版タイプ | VoR | |||||
| 出版タイプResource | http://purl.org/coar/version/c_970fb48d4fbd8a85 | |||||
