Literature DB >> 19540115

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

Gabriella Dessole1, Danila Branca, Federica Ferrigno, Olaf Kinzel, Ester Muraglia, Maria Cecilia Palumbi, Michael Rowley, Sergio Serafini, Christian Steinkühler, Philip Jones.   

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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Year:  2009        PMID: 19540115     DOI: 10.1016/j.bmcl.2009.05.112

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  3 in total

1.  Diamine Ligands in Copper-Catalyzed Reactions.

Authors:  David S Surry; Stephen L Buchwald
Journal:  Chem Sci       Date:  2010       Impact factor: 9.825

2.  HARC as an open-shell strategy to bypass oxidative addition in Ullmann-Goldberg couplings.

Authors:  Marissa N Lavagnino; Tao Liang; David W C MacMillan
Journal:  Proc Natl Acad Sci U S A       Date:  2020-08-17       Impact factor: 11.205

3.  Syntheses of 1-Aryl-5-nitro-1H-indazoles and a General One-Pot Route to 1-Aryl-1H-indazoles.

Authors:  Joel K Annor-Gyamfi; Krishna Kumar Gnanasekaran; Richard A Bunce
Journal:  Molecules       Date:  2018-03-16       Impact factor: 4.411

  3 in total

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