Chen Qi-Feng, Wang Feng-Peng, Liu Xiao-Yu
Key Laboratory of Drug Targeting and Drug Delivery, Systems of the Ministry of Education and Department of Chemistry of Medicinal Natural Products, West China School of Pharmacy, Sichuan University, Chengdu 610041 (P. R. China).
Chemistry. 2015 Jun 8;21(24):8946-50. doi: 10.1002/chem.201500839. Epub 2015 May 7.
The development of new drugs calls for large collections of diverse molecules with considerable complexity. Ring distortion of natural products provides an efficient and facile approach to access new architectures with intriguing biological activities, by harnessing their inherent complexity. In this study, such a strategy has been explored on an abundant C19 -diterpenoid alkaloid, deltaline, enabling the synthesis of 32 new derivatives bearing a broad spectrum of unique scaffolds. Extensive spectroscopic studies including X-ray crystallographic analyses strongly supported the structures of the obtained novel skeletons, which present comparable opportunities with the great contributions made by nature for discovery of new lead compounds.
新药的研发需要大量收集具有相当复杂性的多样分子。天然产物的环畸变通过利用其固有的复杂性，为获取具有有趣生物活性的新结构提供了一种高效且简便的方法。在本研究中，已对一种丰富的C19 -二萜生物碱——去氢鄂尔多斯碱探索了这样一种策略，从而能够合成32种带有一系列独特骨架的新衍生物。包括X射线晶体学分析在内的广泛光谱研究有力地支持了所获得的新型骨架的结构，这些骨架为发现新的先导化合物提供了与大自然所做巨大贡献相当的机会。
