Home > Publications database > Multimechanism biological profiling of tetrahydro-β-carboline analogues as selective HDAC6 inhibitors for the treatment of Alzheimer's disease. > print

001     291284
005     20251015124913.0
024 7 _ |a 10.1016/j.ejmech.2024.116624
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100 1 _ |a Liang, Ting
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245 _ _ |a Multimechanism biological profiling of tetrahydro-β-carboline analogues as selective HDAC6 inhibitors for the treatment of Alzheimer's disease.
260 _ _ |a Amsterdam [u.a.]
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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.
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650 _ 7 |a Alzheimer's disease
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650 _ 7 |a HDAC6 inhibitor
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650 _ 7 |a Multimechanism
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650 _ 7 |a Selectivity
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650 _ 7 |a Tetrahydrocarboline
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700 1 _ |a Liu, Shiru
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700 1 _ |a Dang, Baiyun
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700 1 _ |a Luan, Xiaofa
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700 1 _ |a Guo, Yifan
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700 1 _ |a Steimbach, Raphael
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700 1 _ |a Miller, Aubry
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700 1 _ |a Hu, Jiadong
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700 1 _ |a Lu, Long
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700 1 _ |a Yue, Peiyu
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700 1 _ |a Wang, Ruotian
|b 10
700 1 _ |a Zheng, Meng
|b 11
700 1 _ |a Gao, Jinming
|b 12
700 1 _ |a Yin, Xia
|b 13
700 1 _ |a Chen, Xin
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773 _ _ |a 10.1016/j.ejmech.2024.116624
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|t European journal of medicinal chemistry
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