Stereoselective Synthesis of F-Ring Saturated Estrone-Derived Inhibitors of Hedgehog Signaling Based on Cyclopamine

Previous work in this laboratory established that the readily available F-ring aromatic analog of cyclopamine is a highly potent inhibitor of Hedgehog signaling. The synthesis and biological evaluation of two F-ring saturated analogs that are more potent than the F-ring aromatic structure are reported.

本实验室既往研究工作证实，环巴胺（cyclopamine）的易得F环芳香类似物是一种强效的Hedgehog信号通路抑制剂。本文报道了两种活性优于该F环芳香结构的F环饱和类似物的合成与生物学评价。