Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2018-03-23 , DOI: 10.1016/j.bmcl.2018.03.065 Hang Chu 1 , Georg Dünstl 2 , Jakob Felding 2 , Phil S Baran 1
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Thapsigargin (3) is a potent inhibitor of the SERCA-pump protein, with potential for application in a variety of medicinal areas. The efficient and scalable syntheses of thapsigargin (3) and nortrilobolide (2) have been disclosed previously. To demonstrate the modularity of the previous routes, three natural products (compounds 6, 13, 15) and four analogs (compounds 17–20) have been divergently prepared from a common building block featuring varied acyl chains at the C2, C3, and C8 positions. Biological tests revealed that all of the compounds prepared displayed promising activity profiles.
中文翻译：
毒胡萝卜素类似物的不同合成
Thapsigargin ( 3 ) 是 SERCA 泵蛋白的有效抑制剂，具有在多种医学领域应用的潜力。之前已经公开了毒胡萝卜素( 3 )和去甲三叶内酯( 2 )的高效且可规模化的合成。为了证明先前路线的模块化，三种天然产物（化合物6 、 13 、 15 ）和四种类似物（化合物17 – 20 ）已从 C2、C3 和 C8 处具有不同酰基链的共同构建块中不同地制备出来。职位。生物学测试表明，所有制备的化合物都显示出有希望的活性特征。
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