Synthesis and structure-activity relationships of novel indazolyl glucocorticoid receptor partial agonists.
| Autor: | Gilmore JL; Research and Development, Bristol-Myers Squibb Company, Princeton, NJ 08543-4000, USA. john.gilmore@bms.com, Sheppeck JE 2nd, Wang J, Dhar TG, Cavallaro C, Doweyko AM, Mckay L, Cunningham MD, Habte SF, Nadler SG, Dodd JH, Somerville JE, Barrish JC |
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| Jazyk: | angličtina |
| Zdroj: | Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2013 Oct 01; Vol. 23 (19), pp. 5448-51. Date of Electronic Publication: 2013 Jul 04. |
| DOI: | 10.1016/j.bmcl.2013.06.085 |
| Abstrakt: | 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. (Copyright © 2013 Elsevier Ltd. All rights reserved.) |
| Databáze: | MEDLINE |
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