Bioorg Med Chem Lett. 2009 Aug 1;19(15):4191-5. Epub 2009 Jun 2.

Discovery of N-[(1-aryl-1H-indazol-5-yl)methyl]amides derivatives as smoothened antagonists for inhibition of the hedgehog pathway.

Dessole G, Branca D, Ferrigno F, Kinzel O, Muraglia E, Palumbi MC, Rowley M, Serafini S, Steinkühler C, Jones P.

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IRBM-Merck Research Laboratories Rome, Via Pontina km 30,600, Pomezia 00040, Rome, Italy. gabriella_dessole@merck.com

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.

PMID:: 19540115; [PubMed - indexed for MEDLINE]

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Discovery of N-[(1-aryl-1H-indazol-5-yl)methyl]amides derivatives as smoothened ...
Discovery of N-[(1-aryl-1H-indazol-5-yl)methyl]amides derivatives as smoothened antagonists for inhibition of the hedgehog pathway.
Bioorg Med Chem Lett. 2009 Aug 1 ;19(15):4191-5. Epub 2009 Jun 2 .

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