Wutz, D. and Gluhacevic, D. and Chakrabarti, A. and Schmidtkunz, K. and Robaa, D. and Erdmann, F. and Romier, C. and Sippl, W. and Jung, M. and Koenig, B. (2017) Photochromic histone deacetylase inhibitors based on dithienylethenes and fulgimides. ORGANIC & BIOMOLECULAR CHEMISTRY, 15 (22). pp. 4882-4896. ISSN 1477-0520, 1477-0539
Full text not available from this repository. (Request a copy)Abstract
Histone deacetylases (HDACs) play a crucial role in numerous biological processes and therefore are targeted in anticancer research and in the field of epigenetics. Dithienylethenes (DTEs) and fulgimides were functionalized with hydroxamic acids, which is a known moiety binding to zinc dependent HDACs, to gain photoswitchable HDAC inhibitors. The new DTE based inhibitors showed moderate photochromic properties in polar solvents and the inhibitory activity changes up to a factor of four. The photochromic performance of the prepared fulgimide inhibitors was very good, even in aqueous buffer. They achieved a maximum threefold difference in inhibitory activity. Docking experiments using the crystal structures of the tested enzymes gave a rationale for the observed moderate differences in the activities of the inhibitors.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | ALPHA-CHYMOTRYPSIN ACTIVITY; ENABLE OPTICAL CONTROL; BY-PRODUCT FORMATION; HDAC INHIBITORS; DIARYLETHENE DERIVATIVES; ENZYME-INHIBITORS; VISIBLE-LIGHT; AZOBENZENE; PHOTOSWITCH; RECEPTORS; |
| Subjects: | 500 Science > 540 Chemistry & allied sciences |
| Divisions: | Chemistry and Pharmacy > Institut für Organische Chemie > Lehrstuhl Prof. Dr. Burkhard König |
| Depositing User: | Dr. Gernot Deinzer |
| Date Deposited: | 14 Dec 2018 13:10 |
| Last Modified: | 26 Feb 2019 08:12 |
| URI: | https://pred.uni-regensburg.de/id/eprint/698 |
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