1186293-03-7Relevant academic research and scientific papers
UNSATURATED BICYCLIC HETEROCYCLIC DERIVATIVES AS SMO ANTAGONISTS
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Page/Page column 36; 37, (2010/08/08)
The present invention relates to compounds of formula (I); and pharmaceutically acceptable salts or tautomers thereof which are inhibitors of the Sonic Hedgehog pathway, in particular Smo antagonists. Thus the compounds of this invention are useful for th
Discovery of N-[(1-aryl-1H-indazol-5-yl)methyl]amides derivatives as smoothened antagonists for inhibition of the hedgehog pathway
Dessole, Gabriella,Branca, Danila,Ferrigno, Federica,Kinzel, Olaf,Muraglia, Ester,Palumbi, Maria Cecilia,Rowley, Michael,Serafini, Sergio,Steinkuehler, Christian,Jones, Philip
scheme or table, p. 4191 - 4195 (2010/04/24)
We report the synthesis and biological evaluation of N-[(1-aryl-1H-indazol-5-yl)methyl]amide derivatives as Smoothened antagonists and inhibitors of the Hedgehog pathway. Identification of the lead structure 1 by HTS, followed by SAR study on the amide and aryl portions led to the discovery of antagonists with nanomolar activity.
