Article

Structure-based design of thienobenzoxepin inhibitors of PI3-kinase.

Discovery Chemistry, Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, USA.
Bioorganic & medicinal chemistry letters (impact factor: 2.65). 07/2011; 21(13):4054-8. DOI:10.1016/j.bmcl.2011.04.124 pp.4054-8
Source: PubMed

ABSTRACT Starting from thienobenzopyran HTS hit 1, co-crystallization, molecular modeling and metabolic analysis were used to design potent and metabolically stable inhibitors of PI3-kinase. Compound 15 demonstrated PI3K pathway suppression in a mouse MCF7 xenograft model.

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Keywords

co-crystallization
 
Compound 15
 
metabolic analysis
 
metabolically stable inhibitors
 
mouse MCF7 xenograft model
 

Steven T Staben