近日，南开大学鲁照永团队研究了1'-差向异构-septosones B和C的全合成及抗癌活性新化合物的发现。2025年6月18日出版的《中国化学》杂志发表了这项成果。

Septosones B和C是一对多环阿瓦烷型萜类酚，其拥有独特的螺[4.5]癸烷骨架，并表现出显著的生物活性。研究组报道了1'-差向异构-septosones B和C的全合成，其关键步骤是通过一个不寻常的立体专一性1,2-烷基迁移反应，将一个6/6稠合双烯酮叔醇转化为螺[4.5]烯二酮骨架。

更重要的是，通过对合成高级中间体的生物活性分析，发现两种新化合物对Hep G2、MV-4-11和MOLT-4细胞系表现出强效的抗癌活性，其IC₅₀值低至2.1 μM。

附：英文原文

Title: Total Synthesis of 1'-epi-Septosones B and C and Discovery of Novel Compounds with Anti-Cancer Activity

Author: Qunlong Zhang, Jingyi Kang, Tiancheng Tan, Guanjun Dong, Jianwei Chen, Zhaoyong Lu

Issue&Volume: 2025-06-18

Abstract: Septosones B and C are a pair of polycyclic avarane-type meroterpenoids which possess a distinctive spiro[4.5]decane backbone and exhibit promising biological activity. We report here the total synthesis of 1'-epi-septosones B and C through an unusual stereospecific 1,2-alkyl migration of a 6/6-fused dienone tertiary alcohol to a spiro[4.5]enedione scaffold. More importantly, two new compounds were found to exhibit potent anti-cancer activity against Hep G2, MV-4-11, and MOLT-4 cell lines with IC50 values as low as 2.1 μM through bioactivity profiling of the synthetic advanced intermediates.

DOI: 10.1002/cjoc.70121

Source: https://onlinelibrary.wiley.com/doi/10.1002/cjoc.70121