[摘要]:antagonists derived from cyclopamine. The acid sensitive D-ring of cyclopamine was homologated utilizing a sequence of chemoselective cyclopropanation and stereoselective acid-catalyzed rearrangement. Further modification of the A/B-ring homoallylic alc. to the conjugated ketone led to the discovery of new cyclopamine analogs, e.g. I, with ranging from 10 to 1000 nM.