609806-82-8Relevant articles and documents
Optimization of drug-like properties of nonsteroidal glucocorticoid mimetics and identification of a clinical candidate
Harcken, Christian,Riether, Doris,Liu, Pingrong,Razavi, Hossein,Patel, Usha,Lee, Thomas,Bosanac, Todd,Ward, Yancey,Ralph, Mark,Chen, Zhidong,Souza, Donald,Nelson, Richard M.,Kukulka, Alison,Fadra-Khan, Tazmeen N.,Zuvela-Jelaska, Ljiljana,Patel, Mita,Thomson, David S.,Nabozny, Gerald H.
supporting information, p. 1318 - 1323 (2015/01/09)
A series of nonsteroidal dissociated glucocorticoid receptor agonists was optimized for drug-like properties such as cytochrome P450 inhibition, metabolic stability, aqueous solubility, and hERG ion channel inhibition. This effort culminated in the identification of the clinical candidate compound (R)-39.
Nonsteroidal dissociated glucocorticoid agonists containing azaindoles as steroid A-ring mimetics
Riether, Doris,Harcken, Christian,Razavi, Hossein,Kuzmich, Daniel,Gilmore, Thomas,Bentzien, J?rg,Pack, Edward J.,Souza, Donald,Nelson, Richard M.,Kukulka, Alison,Fadra, Tazmeen N.,Zuvela-Jelaska, Ljiljana,Pelletier, Josephine,Dinallo, Roger,Panzenbeck, Mark,Torcellini, Carol,Nabozny, Gerald H.,Thomson, David S.
experimental part, p. 6681 - 6698 (2010/12/19)
Syntheses and structure-activity relationships (SAR) of nonsteroidal glucocorticoid receptor (GR) agonists are described. These compounds contain azaindole moieties as A-ring mimetics and display various degrees of in vitro dissociation between gene trans
Identification of dissociated non-steroidal glucocorticoid receptor agonists
Kuzmich, Daniel,Kirrane, Tom,Proudfoot, John,Bekkali, Younes,Zindell, Renee,Beck, Laura,Nelson, Richard,Shih, Cheng-Kon,Kukulka, Alison J.,Paw, Zofia,Reilly, Patty,Deleon, Rodney,Cardozo, Mario,Nabozny, Gerald,Thomson, David
, p. 5025 - 5031 (2008/02/11)
A new series of ligands for the glucocorticoid receptor (GR) is described. SAR development was guided by docking 3 into the GR active site and optimizing an unsubstituted phenyl ring for key interactions found in the steroid A-ring binding pocket. To iden