Academic Journal
Discovery of tetrahydroisoquinoline derivatives as selective histone deacetylase 6 inhibitors with neurite outgrowth-promoting activities and neuroprotective activities.
| Τίτλος: | Discovery of tetrahydroisoquinoline derivatives as selective histone deacetylase 6 inhibitors with neurite outgrowth-promoting activities and neuroprotective activities. |
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| Συγγραφείς: | Liu S; Shaanxi Key Labotory of Natural Products & Chemical Biology, College of Chemistry & Pharmacy, Northwest A&F University, Yangling 712100, PR China., Dang B; Shaanxi Key Labotory of Natural Products & Chemical Biology, College of Chemistry & Pharmacy, Northwest A&F University, Yangling 712100, PR China., Kang Z; Shaanxi Key Labotory of Natural Products & Chemical Biology, College of Chemistry & Pharmacy, Northwest A&F University, Yangling 712100, PR China., Wei R; Shaanxi Key Labotory of Natural Products & Chemical Biology, College of Chemistry & Pharmacy, Northwest A&F University, Yangling 712100, PR China., Yang Z; College of Medicinal and Chemical Engineering, Shaanxi A&F Technology University, Yangling, Shannxi 712100, PR China., Guo X; College of Medicinal and Chemical Engineering, Shaanxi A&F Technology University, Yangling, Shannxi 712100, PR China., Shao F; College of Medicinal and Chemical Engineering, Shaanxi A&F Technology University, Yangling, Shannxi 712100, PR China., Li Z; Department of Student Affairs, The Second Affiliated Hospital of Xi'an Jiaotong University, Xi'an 710004, Shaanxi, PR China., Xing L; Guangxi Key Laboratory of Urban Water Environment, College of Chemistry and Environmental Engineering, Baise University, Baise 533000, PR China. Electronic address: 1094895479@qq.com., Hu J; College of Medicinal and Chemical Engineering, Shaanxi A&F Technology University, Yangling, Shannxi 712100, PR China. Electronic address: hujiadong@aliyun.com., Chen X; Shaanxi Key Labotory of Natural Products & Chemical Biology, College of Chemistry & Pharmacy, Northwest A&F University, Yangling 712100, PR China. Electronic address: chenxin1888@nwsuaf.edu.cn. |
| Πηγή: | Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2026 Jul; Vol. 136, pp. 130593. Date of Electronic Publication: 2026 Feb 17. |
| Τύπος έκδοσης: | Journal Article |
| Γλώσσα: | English |
| Στοιχεία περιοδικού: | Publisher: Elsevier Science Ltd Country of Publication: England NLM ID: 9107377 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1464-3405 (Electronic) Linking ISSN: 0960894X NLM ISO Abbreviation: Bioorg Med Chem Lett Subsets: MEDLINE |
| Imprint Name(s): | Publication: Oxford : Elsevier Science Ltd Original Publication: Oxford ; New York : Pergamon Press, c1991- |
| Ιατρικοί όροι (MeSH): | Histone Deacetylase Inhibitors*/pharmacology , Histone Deacetylase Inhibitors*/chemistry , Histone Deacetylase Inhibitors*/chemical synthesis , Neuroprotective Agents*/pharmacology , Neuroprotective Agents*/chemistry , Neuroprotective Agents*/chemical synthesis , Histone Deacetylase 6*/antagonists & inhibitors , Histone Deacetylase 6*/metabolism , Tetrahydroisoquinolines*/pharmacology , Tetrahydroisoquinolines*/chemistry , Tetrahydroisoquinolines*/chemical synthesis , Neuronal Outgrowth*/drug effects , Neurites*/drug effects , Drug Discovery*, Histone Deacetylases/metabolism ; Animals ; Rats ; Structure-Activity Relationship ; PC12 Cells ; Molecular Structure ; Humans ; Dose-Response Relationship, Drug |
| Περίληψη: | Recently, histone deacetylase 6 (HDAC6) has attracted considerable attention for its potential in treating neurodegenerative disorders. In this paper, a series of tetrahydroisoquinoline derivatives were designed and synthesized as selective HDAC6 inhibitors. 4-((7-chloro-3, 4-dihydroisoquinolin-2(1H)-yl)methyl)-3-fluoro-N-hydroxybenzamide (8g), the most promising compound, potently inhibited HDAC6 (IC (Copyright © 2024. Published by Elsevier Ltd.) |
| Competing Interests: | Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper. |
| Contributed Indexing: | Keywords: HDAC6 inhibitor; Neurite outgrowth; Neuroprotective; Selectivity; THIQ |
| Substance Nomenclature: | 0 (Histone Deacetylase Inhibitors) 0 (Neuroprotective Agents) EC 3.5.1.98 (Histone Deacetylase 6) 0 (Tetrahydroisoquinolines) EC 3.5.1.98 (HDAC6 protein, human) EC 3.5.1.98 (Histone Deacetylases) |
| Entry Date(s): | Date Created: 20260219 Date Completed: 20260708 Latest Revision: 20260708 |
| Update Code: | 20260708 |
| DOI: | 10.1016/j.bmcl.2026.130593 |
| PMID: | 41713755 |
| Βάση Δεδομένων: | MEDLINE |
| ISSN: | 1464-3405 |
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| DOI: | 10.1016/j.bmcl.2026.130593 |