2. Academic Validation
  3. Potent agonists of the Hedgehog signaling pathway

Potent agonists of the Hedgehog signaling pathway

  • Bioorg Med Chem Lett. 2009 Aug 1;19(15):4308-11. doi: 10.1016/j.bmcl.2009.05.096.
Shirley A Brunton 1,  John H A Stibbard,  Lee L Rubin,  Oivin M Guicherit,  Lawrence I Kruse,  Stephen Price,  Raffaella di Lucrezia,  Colin H MacKinnon,  Alaric Avery,  Yvonne Park,  Danielle Buxton,  Edward A Boyd
Affiliations

Affiliation

PMID: 19500978 DOI: 10.1016/j.bmcl.2009.05.096
Abstract

A family of biaryl substituted 1,4-diaminocyclohexanamides of 3-chlorobenzothiophene-2-carboxylic acid is reported as picomolar modulators of Hedgehog protein function. SAR for the 1,4-diaminocyclohexane group is shown to be exquisitely sensitive to substitution on the 4-amino group, and SAR for the 3-chlorobenzothiophene group is highly specific. Preliminary SAR studies of the biaryl substituent led to a picomolar compound with in vivo activity.

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