609849-80-1Relevant 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
