Graduate School of Pharmaceutical Sciences, Kyushu University, 3-1-1 Maidashi, Higashi-ku, Fukuoka 812-8582, Japan.
RIKEN Cluster for Pioneering Research, 2-1 Hirosawa, Wako-shi, Saitama 351-0198, Japan.
Org Lett. 2020 Nov 20;22(22):8877-8881. doi: 10.1021/acs.orglett.0c03255. Epub 2020 Oct 30.
We designed and synthesized a series of derivatives containing the right-side DFGH-ring structure of physalin-type natural products, decorated with a hydrophobic substituent. The synthetic scheme utilizes a highly efficient, one-pot protocol for simultaneous construction of the GH-ring system, promoted by HF/pyridine. Among the compounds synthesized, inhibited TNF-α-stimulated NF-κB activation with similar potency to physalin B.
我们设计并合成了一系列含有半边杯苋烷型天然产物的 DFGH-环结构的衍生物，并在其基础上修饰了疏水性取代基。该合成方案利用高效、一锅法策略，在 HF/吡啶的促进下同时构建 GH-环系统。在所合成的化合物中，化合物 对 TNF-α 刺激的 NF-κB 激活具有与杯苋醇 B 相似的抑制活性。
