Potent Hydrazide-Based HDAC Inhibitors with a Superior Pharmacokinetic Profile for Efficient Treatment of Acute Myeloid Leukemia In Vivo
| Autor: | Yuqi Jiang, Jie Xu, Kairui Yue, Chao Huang, Mengting Qin, Dongyu Chi, Qixin Yu, Yue Zhu, Xiaohan Hou, Tongqiang Xu, Min Li, C. James Chou, Xiaoyang Li |
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| Rok vydání: | 2021 |
| Předmět: |
Mice
Inbred BALB C Mice Nude Antineoplastic Agents Apoptosis Xenograft Model Antitumor Assays Histone Deacetylase Inhibitors Molecular Docking Simulation Leukemia Myeloid Acute Mice Structure-Activity Relationship Hydrazines Drug Design Drug Discovery Tumor Cells Cultured Animals Humans Molecular Medicine Female Tissue Distribution Cell Proliferation |
| Zdroj: | Journal of Medicinal Chemistry. 65:285-302 |
| ISSN: | 1520-4804 0022-2623 |
| DOI: | 10.1021/acs.jmedchem.1c01472 |
| Popis: | As "Michael acceptors" may induce promiscuous responses in mammalian cells by reacting with various proteins, we modified the cinnamamide of our previous hydrazide-based HDAC inhibitors (HDACIs) to deactivate the Michael reaction. Representative compound |
| Databáze: | OpenAIRE |
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