School of Life and Environmental Sciences, Deakin University, Waurn Ponds, 3216, Australia.
Chem Commun (Camb). 2020 Jun 25;56(50):6866-6869. doi: 10.1039/d0cc01251c. Epub 2020 May 20.
An efficient and functional group tolerant route to access hydroxy 1,8-naphthalimides has been used to synthesise a range of mono- and disubstituted hydroxy-1,8-naphthalimides with fluorescence emissions covering the visible spectrum. The dialkoxy substituted compounds prepared possess high quantum yields (up to 0.95) and long fluorescent lifetimes (up to 14 ns). The method has been used to generate scriptaid analogues that successfully inhibit HDAC6 in vitro with tubulin acetylation assays confirming that these compounds are more effective than tubastatin.
已采用一种高效且官能团容忍的方法来合成羟基 1,8-萘酰亚胺，该方法可用于合成一系列具有荧光发射覆盖可见光谱的单取代和二取代的羟基-1,8-萘酰亚胺。所制备的二烷氧基取代化合物具有高量子产率（高达 0.95）和长荧光寿命（高达 14 ns）。该方法已用于生成 scriptaid 类似物，这些类似物在体外通过微管蛋白乙酰化测定成功抑制了 HDAC6，证实这些化合物比 tubastatin 更有效。
