Wender Paul A, Billingsley Kelvin L
Department of Chemistry, Department of Chemical and Systems Biology, Stanford University, Stanford, CA 94305-5080, USA, Fax +1(650)7250259.
Department of Radiology, Stanford University School of Medicine, Stanford, CA 94305-5105, USA.
Synthesis (Stuttg). 2013;45(13):1815-1824. doi: 10.1055/s-0033-1338860.
The design, synthesis, and biological evaluation of a novel class of C13-diversified bryostatin analogues are described. An innovative and general strategy based on a Prins macrocyclization-nucleophilic trapping cascade was used to achieve late-stage diversification. In vitro analysis of selected library members revealed that modification at the C13 position of the bryostatin scaffold can be used as a diversification handle to regulate biological activity.
本文描述了一类新型C13多样化苔藓抑素类似物的设计、合成及生物学评价。基于普林斯大环化-亲核捕获级联反应的创新通用策略被用于实现后期多样化。对所选文库成员的体外分析表明，苔藓抑素支架C13位的修饰可作为调节生物活性的多样化手段。
