Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10596354 | Bioorganic & Medicinal Chemistry Letters | 2009 | 5 Pages |
Abstract
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.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Gabriella Dessole, Danila Branca, Federica Ferrigno, Olaf Kinzel, Ester Muraglia, Maria Cecilia Palumbi, Michael Rowley, Sergio Serafini, Christian Steinkühler, Philip Jones,