Abstract
Abstract Signal transducer and activator of transcription 3 (Stat3) protein is an oncogenic transcription factor that exhibits aberrant functioning in many types human cancer. Constitutive Stat3 activation causes over-expression of anti-apoptotic proteins and makes cancer cells resistant to natural apoptotic processes. Inhibiting Stat3 reduces the expression of anti-apoptotic proteins and can selectively kill cancerous cells. We have identified several salicylic acid based inhibitors of Stat3 that show potent activity in vitro and in whole cell assays. In silico docking studies have revealed S3I-201, a known Stat3 inhibitor, exhibits incomplete occupation of Stat3's SH2 domain. A thorough structure activity relationship study has provided a series of compounds that more completely occupy Stat3's SH2 domain and show potent and highly selective activity against Stat3 and a variety of human cancers. Inhibitor design, synthesis, in vitro and in vivo assays and preliminary metabolic studies will be discussed. Citation Information: Cancer Res 2009;69(23 Suppl):C40.
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