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Synthesis of DFGH-Ring Derivatives of Physalins via One-Pot Construction of GH-Ring and Evaluation of Their NF-κB-Inhibitory Activity
Organic Letters ( IF 5.2 ) Pub Date : 2020-10-30 , DOI: 10.1021/acs.orglett.0c03255
Makoto Yoritate 1 , Yuki Morita 1 , Manuel Gemander 2 , Masaki Morita 1, 2 , Tomohiro Yamashita 1 , Mikiko Sodeoka 2, 3 , Go Hirai 1, 2, 3
Affiliation  

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, 5d inhibited TNF-α-stimulated NF-κB activation with similar potency to physalin B.

中文翻译:

通过一锅法构建 GH 环合成酸碱的 DFGH 环衍生物并评价它们的 NF-κB 抑制活性

我们设计并合成了一系列包含右侧 DFGH 环结构的酸洗素型天然产物的衍生物,并带有疏水取代基。该合成方案利用高效的一锅法同时构建 GH 环系统,由 HF/吡啶促进。在合成的化合物中,5d抑制 TNF-α 刺激的 NF-κB 活化,其效力与酸蚀灵 B 相似。
更新日期:2020-11-21
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