2. Academic Validation
  3. Synthesis and structure-activity relationships of novel indazolyl glucocorticoid receptor partial agonists

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

  • Bioorg Med Chem Lett. 2013 Oct 1;23(19):5448-51. doi: 10.1016/j.bmcl.2013.06.085.
John L Gilmore 1,  James E Sheppeck 2nd,  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
Affiliations

Affiliation

  • 1 Research and Development, Bristol-Myers Squibb Company, Princeton, NJ 08543-4000, USA. john.gilmore@bms.com
PMID: 23916594 DOI: 10.1016/j.bmcl.2013.06.085
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.

Keywords

Dissociated; GR agonist; Glucocortocoids; Selective GR agonist.

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