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Development of UTX-121 and its derivatives as novel matrix metalloproteinase-2/9 inhibitors using celecoxib as a lead compound
https://tokushima-u.repo.nii.ac.jp/records/2009841
https://tokushima-u.repo.nii.ac.jp/records/2009841c0e85447-fada-45ba-b020-2c1719464906
| 名前 / ファイル | ライセンス | アクション |
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k3576_abstract.pdf (60.1 KB)
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k3576_review.pdf (47.4 KB)
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k3576_fulltext.pdf (1.12 MB)
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| Item type | 文献 / Documents(1) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| 公開日 | 2022-04-28 | |||||||||
| アクセス権 | ||||||||||
| アクセス権 | open access | |||||||||
| 資源タイプ | ||||||||||
| 資源タイプ識別子 | http://purl.org/coar/resource_type/c_db06 | |||||||||
| 資源タイプ | doctoral thesis | |||||||||
| 出版タイプ | ||||||||||
| 出版タイプ | NA | |||||||||
| 出版タイプResource | http://purl.org/coar/version/c_be7fb7dd8ff6fe43 | |||||||||
| タイトル | ||||||||||
| タイトル | Development of UTX-121 and its derivatives as novel matrix metalloproteinase-2/9 inhibitors using celecoxib as a lead compound | |||||||||
| 言語 | en | |||||||||
| タイトル別表記 | ||||||||||
| その他のタイトル | Celecoxibをリードとした新規MMP-2/9阻害剤UTX-121およびその誘導体の開発 | |||||||||
| 言語 | ja | |||||||||
| 著者 |
山花, 啓梨
× 山花, 啓梨
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| 抄録 | ||||||||||
| 内容記述タイプ | Abstract | |||||||||
| 内容記述 | Matrix metalloproteinases (MMP)-2/9 are closely associated with cancer malignancy, and it has been considered that the inhibition of these MMPs may be beneficial for enhancing the antitumor and antimetastatic activities of agents. In addition, celecoxib, a COX-2 selective inhibitor, has been reported to have a poor MMPs inhibitory activity, suggesting that it is a very promising drug as an anticancer and antimetastatic agent. We have revealed that UTX-121, which was converted the sulfonamide moiety of celecoxib into a methyl ester, significantly suppressed MT1-MMP-mediated MMP-2 activation and MMP-9 production. Furthermore, UTX-121 also inhibited the migration and invasion of cancer cells. We then searched for compounds with higher MMPs inhibitory activity using a structure-activity relationship (SAR) method based on UTX-121 as a lead compound. Among them, compounds 9c and 10c, in which the methyl moiety of the p-tolyl group in UTX-121 was substituted with F and Cl, showed higher antitumor and MMPs inhibitory activities than UTX-121. These findings suggest that compounds 9c and 10c could be potential lead compounds for the development of potent MMPs inhibitors. | |||||||||
| 言語 | en | |||||||||
| キーワード | ||||||||||
| 言語 | en | |||||||||
| 主題Scheme | Other | |||||||||
| 主題 | matrix metalloproteinase-2/9 | |||||||||
| キーワード | ||||||||||
| 言語 | en | |||||||||
| 主題Scheme | Other | |||||||||
| 主題 | celecoxib | |||||||||
| キーワード | ||||||||||
| 言語 | en | |||||||||
| 主題Scheme | Other | |||||||||
| 主題 | antitumor | |||||||||
| キーワード | ||||||||||
| 言語 | en | |||||||||
| 主題Scheme | Other | |||||||||
| 主題 | antimetastasis | |||||||||
| 書誌情報 |
発行日 2022-03-01 |
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| 備考 | ||||||||||
| 言語 | ja | |||||||||
| 値 | 内容要旨・審査要旨・論文本文の公開 学位授与者所属 : 徳島大学大学院先端技術科学教育部（物質生命システム工学専攻） |
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| 言語 | ||||||||||
| 言語 | eng | |||||||||
| 報告番号 | ||||||||||
| 学位授与番号 | 甲第3576号 | |||||||||
| 学位記番号 | ||||||||||
| 言語 | ja | |||||||||
| 値 | 甲先第418号 | |||||||||
| 学位授与年月日 | ||||||||||
| 学位授与年月日 | 2022-03-01 | |||||||||
| 学位名 | ||||||||||
| 言語 | ja | |||||||||
| 学位名 | 博士（工学） | |||||||||
| 学位授与機関 | ||||||||||
| 言語 | ja | |||||||||
| 学位授与機関名 | 徳島大学 | |||||||||
