2020年11月11日
2-Naphthol Moiety of Neocarzinostatin Chromophore as a Novel Protein-Photodegrading Agent and Its Application as a H<inf>2</inf>O<inf>2</inf>-Activatable Photosensitizer
Chemistry - A European Journal
- ,
- ,
- ,
- 巻
- 26
- 号
- 63
- 開始ページ
- 14351
- 終了ページ
- 14358
- 記述言語
- 掲載種別
- 研究論文(学術雑誌)
- 出版者・発行元
- Wiley-VCH
© 2020 Wiley-VCH GmbH A 2-naphthol derivative 2 corresponding to the aromatic ring moiety of neocarzinostatin chromophore was found to degrade proteins under photo-irradiation with long-wavelength UV light without any additives under neutral conditions. Structure–activity relationship studies of the derivative revealed that methylation of the hydroxyl group at the C2 position of 2 significantly suppressed its photodegradation ability. Furthermore, a purpose-designed synthetic tumor-related biomarker, a H2O2-activatable photosensitizer 8 possessing a H2O2-responsive arylboronic ester moiety conjugated to the hydroxyl group at the C2 position of 2, showed significantly lower photodegradation ability compared to 2. However, release of the 2 from 8 by reaction with H2O2 regenerated the photodegradation ability. Compound 8 exhibited selective photo-cytotoxicity against high H2O2-expressing cancer cells upon irradiation with long-wavelength UV light.
- ID情報
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- ISSN : 0947-6539