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Bioorg Med Chem Lett. 2009 Aug 1;19(15):4191-5. doi: 10.1016/j.bmcl.2009.05.112. 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.

Author information

1
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
DOI:
10.1016/j.bmcl.2009.05.112
[Indexed for MEDLINE]

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