- Potential anti-neuroinflammatory NF-кB inhibitors based on 3,4-dihydronaphthalen-1(2H)-one derivatives
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Nuclear factor kappa B (NF-кB) inhibition represents a new therapeutic strategy for the treatment of neuroinflammatory diseases. In this study, a series of 3,4-dihydronaphthalen-1(2H)-one (DHN; 6a-n, 7a-c) derivatives were synthesised and characterised by NMR and HRMS. We assessed the toxicity and anti-neuroinflammatory properties of these compounds and found that 6m showed the greatest anti-neuroinflammatory properties, with relatively low toxicity. Specifically, 6m significantly reduced reactive oxygen species production, down-regulated the expression of NOD-like receptor pyrin domain-containing protein 3 (NLRP3), apoptosis-associated speck-like protein containing a CARD (ASC), and caspase-1 and prevented lipopolysaccharide-stimulated BV2 microglia cells polarisation towards an M1 phenotype. Furthermore, 6m significantly decreased IκBα and NF-кB p65 phosphorylation, thus inhibiting the NF-кB signalling pathway. This suggests that 6m may be explored as a functional anti-neuroinflammatory agent for the treatment of inflammatory diseases in the central nervous system, such as multiple sclerosis, traumatic brain injury, stroke and spinal cord injury.
- Sun, Yue,Zhou, Yan-Qiu,Liu, Yin-Kai,Zhang, Hong-Qin,Hou, Gui-Ge,Meng, Qing-Guo,Hou, Yun
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- Necrostatins regulate apoptosis, necroptosis, and inflammation in cisplatin-induced nephrotoxicity in LLC-PK1 cells
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Acute kidney injury (AKI) is a common clinical problem that is associated with high mortality due to multiple complex mechanisms. Cisplatin is the most important and highly effective chemotherapeutic agent used for the treatment of various solid tumors; h
- Kim, Dong-Wook,Lee, Dahae,Lee, Heesu,Lim Lee, Hye,Sung Kang, Ki,Wook Lee, Jae,Yamabe, Noriko
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- Selectivity in the Aerobic Dearomatization of Phenols: Total Synthesis of Dehydronornuciferine by Chemo- and Regioselective Oxidation
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We describe a selective aerobic oxidation of meta-biaryl phenols that enables rapid access to functionalized phenanthrenes. Aerobic oxidations attract interest due to their efficiency, but remain underutilized in complex molecule settings due to challenge
- Esguerra, Kenneth Virgel N.,Lumb, Jean-Philip
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supporting information
p. 1514 - 1518
(2018/01/27)
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- Discovery of 3,3a,4,5-tetrahydro-2H-benzo[g]indazole containing quinoxaline derivatives as novel EGFR/HER-2 dual inhibitors
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In the present study, twenty-five pyrazole-quinoxaline derivatives (4a-4y) were designed and synthesized, and their biological activity as potential EGFR or HER-2 kinase inhibitors was evaluated. Among them, compound 4l displayed better antiproliferative
- Zong, Xi,Cai, Jin,Chen, Junqing,Sun, Chunlong,Li, Lushen,Ji, Min
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p. 24814 - 24823
(2015/03/30)
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