Synthesis and structure-activity relationships of novel indazolyl glucocorticoid receptor partial agonists

John L. Gilmore, James E. Sheppeck, Jim Wang, T. G.Murali Dhar, Cullen Cavallaro, Arthur M. Doweyko, Lorraine McKay, Mark D. Cunningham, Sium F. Habte, Steven G. Nadler, John H. Dodd, John E. Somerville, Joel C. Barrish

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Abstract

SAR was used to further develop an indazole class of non-steroidal glucocorticoid receptor agonists aided by a GR LBD (ligand-binding domain)-agonist co-crystal structure described in the accompanying paper. Progress towards discovering a dissociated GR agonist guided by human in vitro assays biased the optimization of this compound series towards partial agonists that possessed excellent selectivity against other nuclear hormone receptors.

Original languageEnglish (US)
Pages (from-to)5448-5451
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume23
Issue number19
DOIs
StatePublished - Oct 1 2013

All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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    Gilmore, J. L., Sheppeck, J. E., Wang, J., Dhar, T. G. M., Cavallaro, C., Doweyko, A. M., McKay, L., Cunningham, M. D., Habte, S. F., Nadler, S. G., Dodd, J. H., Somerville, J. E., & Barrish, J. C. (2013). Synthesis and structure-activity relationships of novel indazolyl glucocorticoid receptor partial agonists. Bioorganic and Medicinal Chemistry Letters, 23(19), 5448-5451. https://doi.org/10.1016/j.bmcl.2013.06.085