Synthesis and evaluation of gallocyanine dyes as potential agents for the treatment of Alzheimer's disease and related neurodegenerative tauopathies
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- 作者：Spyros Mpousisa ; 1 ; Savvas Thysiadisa ; 1 ; Nicolaos Avramidisb ; 1 ; Sotirios Katsamakasc ; Spiros Efthimiopoulosb ; efthis@biol.uoa.gr" class="auth_mail" title="E-mail the corresponding author ; Vasiliki Sarlia ; sarli@chem.auth.gr" class="auth_mail" title="E-mail the corresponding author
- 关键词：Gallocyanine ; Phenoxazine ; DKK1 inhibitors ; DKK1/LRP6 interaction inhibitors ; Tau phosphorylation inhibition ; Alzheimer's disease ; Tauopathies
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：27 January 2016
- 年：2016
- 卷：108
- 期：Complete
- 页码：28-38
- 全文大小：1433 K
文摘
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Novel NCI8642 compounds were synthesized as potential LRP/DKK inhibitors.
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Novel inhibitors of LRPs/DKK1 interactions were identified.
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Important features for activity of NCI8642 template have been recognized.
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Gallocyanine dyes exhibit a sufficient physicochemical profile.
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NCI8642 and derivatives inhibit PGJ2-induced tau phosphorylation at serine 396.