1200404-06-3Relevant academic research and scientific papers
Discovery of amide replacements that improve activity and metabolic stability of a bis-amide smoothened antagonist hit
Brown, Matthew L.,Aaron, Wade,Austin, Richard J.,Chong, Angela,Huang, Tom,Jiang, Ben,Kaizerman, Jacob A.,Lee, Gary,Lucas, Brian S.,McMinn, Dustin L.,Orf, Jessica,Rong, Minqing,Toteva, Maria M.,Xu, Guifen,Ye, Qiuping,Zhong, Wendy,Degraffenreid, Michael R.,Wickramasinghe, Dineli,Powers, Jay P.,Hungate, Randall,Johnson, Michael G.
scheme or table, p. 5206 - 5209 (2011/10/09)
A bis-amide antagonist of Smoothened, a seven-transmembrane receptor in the Hedgehog signaling pathway, was discovered via high throughput screening. In vitro and in vivo experiments demonstrated that the bis-amide was susceptible to N-acyl transferase mediated amide scission. Several bioisosteric replacements of the labile amide that maintained in vitro potency were identified and shown to be metabolically stable in vitro and in vivo.
OXAZOLE COMPOUNDS, COMPOSITIONS AND METHODS OF USE
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, (2010/01/07)
The present invention relates generally to compounds represented in Formula (I), pharmaceutical compositions comprising them and methods of treating of diseases or disorders such as cancer.
