Multimechanism biological profiling of tetrahydro-β-carboline analogues as selective HDAC6 inhibitors for the treatment of Alzheimer's disease
With the intensive research on the pathogenesis of Alzheimer's disease (AD), inhibition of HDAC6 appears to be a potential therapeutic approach for AD. In this paper, a series of tetrahydro-β-carboline derivatives with hydroxamic acid group were fast synthesized. Among all, the most potent 15 s...
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| Main Authors: | , , , , , , , , , , , , , |
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| Format: | Article (Journal) |
| Language: | English |
| Published: |
5 September 2024
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| In: |
European journal of medicinal chemistry
Year: 2024, Volume: 275, Pages: 1-18 |
| ISSN: | 1768-3254 |
| DOI: | 10.1016/j.ejmech.2024.116624 |
| Online Access: | Verlag, lizenzpflichtig, Volltext: https://doi.org/10.1016/j.ejmech.2024.116624 Verlag, lizenzpflichtig, Volltext: https://www.sciencedirect.com/science/article/pii/S022352342400504X 
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| Author Notes: | Ting Liang, Shiru Liu, Baiyun Dang, Xiaofa Luan, Yifan Guo, Raphael R. Steimbach, Jiadong Hu, Long Lu, Peiyu Yue, Ruotian Wang, Meng Zheng, Jinming Gao, Xia Yin, Xin Chen |
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| 520 | |a With the intensive research on the pathogenesis of Alzheimer's disease (AD), inhibition of HDAC6 appears to be a potential therapeutic approach for AD. In this paper, a series of tetrahydro-β-carboline derivatives with hydroxamic acid group were fast synthesized. Among all, the most potent 15 selectively inhibited HDAC6 with IC50 of 15.2 nM and markedly increased acetylated alpha-tubulin levels. In cellular assay, 15 showed excellent neurotrophic effect by increasing the expression of GAP43 and Beta-3 tubulin markers. Besides, 15 showed neuroprotective effects in PC12 or SH-SY5Y cells against H2O2 and 6-OHDA injury through activation of Nrf2, catalase and Prx II, and significantly reduced H2O2-induced reactive oxygen species (ROS) production. In vivo, 15 significantly attenuated zebrafish anxiety-like behaviour and memory deficits in a SCOP-induced zebrafish model of AD. To sum up, multifunctional 15 might be a good lead to develop novel tetrahydrocarboline-based agents for the treatment of AD. | ||
| 650 | 4 | |a Alzheimer's disease | |
| 650 | 4 | |a HDAC6 inhibitor | |
| 650 | 4 | |a Multimechanism | |
| 650 | 4 | |a Selectivity | |
| 650 | 4 | |a Tetrahydrocarboline | |
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| 700 | 1 | |a Chen, Xin |e VerfasserIn |4 aut | |
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