奥沙金、山橙酮及其类似物的全合成与抗炎活性评价
Total Synthesis and Anti-Inflammatory Evaluation of Osajin, Scandenone and Analogues.
作者信息
Wang Rui, Ma Ran, Feng Ke, Lu Hongchen, Zhao Wei, Jin Hongzhen
机构信息
State Key Laboratory of Medicinal Chemical Biology, Key Laboratory of Molecular Drug Research and KLMDASR of Tianjin, College of Pharmacy, Nankai University, Tianjin 300350, China.
Tianjin International Joint Academy of Biomedicine, Tianjin 300457, China.
出版信息
Pharmaceuticals (Basel). 2024 Jan 9;17(1):86. doi: 10.3390/ph17010086.
In this study, the total synthesis of osajin, scandenone and their analogues have been accomplished. The key synthetic steps include aldol/intramolecular iodoetherification/elimination sequence reactions and a Suzuki coupling reaction to assemble the tricyclic core, chemoselective propargylation and Claisen rearrangement reactions to obtain natural compounds. In addition, we also designed and synthesized twenty-five natural product analogues. All synthetic compounds were screened for anti-inflammatory activity against tumor necrosis factor-α (TNF-α) and interleukin-6 (IL-6) in lipopolysaccharide (LPS)-stimulated RAW264.7 macrophages. Collectively, Compound and were considered as promising lead compounds for further development.
在本研究中，已完成奥沙金、 scandenenone及其类似物的全合成。关键的合成步骤包括羟醛缩合/分子内碘醚化/消除序列反应以及用于组装三环核心的铃木偶联反应、化学选择性炔丙基化反应和克莱森重排反应以获得天然化合物。此外，我们还设计并合成了25种天然产物类似物。对所有合成化合物进行了筛选，以检测其在脂多糖（LPS）刺激的RAW264.7巨噬细胞中对肿瘤坏死因子-α（TNF-α）和白细胞介素-6（IL-6）的抗炎活性。总体而言，化合物 和 被认为是有进一步开发潜力的先导化合物。
Zotero 插件