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Semisynthetic Cyclopamine Analogues as Potent and Orally Bioavailable Hedgehog Pathway Antagonists.

  作者 Tremblay, Martin R.;Nevalainen, Marta;Nair, Somarajan J.;Porter, James R.;Castro, Alfredo C.;Behnke, Mark L.;Yu, Lin-Chen;Hagel, Margit;White, Kerry;Faia, Kerrie;Grenier, Louis;Campbell, Matthew J.;Cushing, Jill;Woodward, Caroline N.;Hoyt, Jennifer;Foley,  
  选自 期刊  Journal of Medicinal Chemistry;  卷期  2008年51-21;  页码  6646-6649  
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[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.

 
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