Graduate School of Pharmaceutical Sciences, Osaka University, Suita, Osaka, 565-0871, Japan.
Department of Environmental and Molecular Health Sciences, Faculty of Medical and Pharmaceutical Sciences, Kumamoto University, Kumamoto, 862-0973, Japan.
Chemistry. 2023 Aug 4;29(44):e202300677. doi: 10.1002/chem.202300677. Epub 2023 Jul 6.
Structurally simplified analogues of ansellone A, in which the decalin skeleton is replaced with a lipophilic chain, were prepared and their HIV latency-reversing activities biologically evaluated. In particular, two analogues bearing ether and alkenyl side chains, respectively, showed comparable activities to that of ansellone A. Each of the simplified compounds was easily synthesized using Prins cyclisation chemistry.
我们制备了安丝菌素 A 的结构简化类似物,其中十氢萘骨架被亲脂性链取代,并对其逆转 HIV 潜伏活性进行了生物学评价。特别是,分别带有醚和烯基侧链的两种类似物具有与安丝菌素 A 相当的活性。每个简化化合物都可以使用 Prins 环化化学方法轻松合成。