Simeth, Nadja A. and Altmann, Lisa-Marie and Woessner, Nathalie and Bauer, Elisabeth and Jung, Manfred and Koenig, Burkhard (2018) Photochromic Indolyl Fulgimides as Chromo-pharmacophores Targeting Sirtuins. JOURNAL OF ORGANIC CHEMISTRY, 83 (15). pp. 7919-7927. ISSN 0022-3263,
Full text not available from this repository. (Request a copy)Abstract
Sirtuins are involved in epigenetic regulation, the pathogenesis of cancer, and several metabolic and neurodegenerative diseases. Despite being a promising drug target, only one small molecule passed class II clinical trials to date. Deriving a better mechanistic understanding is hence crucial to find new modulators. We previously reported on a series of dithienyl maleimides as photochromic tool compounds. However, their photochromic behavior was limited. To improve the interconversion and stability of both photoisomers, we replaced the dithienyl maleimide with a fulgimide as a photochromic core to result in biologically active compounds reversibly addressable with purple and orange light. We characterize the obtained compounds regarding their spectroscopic properties, their photostability, and binding characteristics toward sirtuins resulting in a fully remote-controllable Sirtuin modulator using visible light as the external stimulant.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | NAD(+)-DEPENDENT HISTONE DEACETYLASES; DIARYLETHENE DERIVATIVES; OPTICAL CONTROL; INHIBITORS; KINASE; LIGHT; PHOTOPHARMACOLOGY; CHROMAN-4-ONE; |
| Subjects: | 500 Science > 540 Chemistry & allied sciences |
| Divisions: | Chemistry and Pharmacy > Institut für Organische Chemie Chemistry and Pharmacy > Institut für Organische Chemie > Lehrstuhl Prof. Dr. Burkhard König |
| Depositing User: | Dr. Gernot Deinzer |
| Date Deposited: | 05 Mar 2020 10:22 |
| Last Modified: | 05 Mar 2020 10:22 |
| URI: | https://pred.uni-regensburg.de/id/eprint/14063 |
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