Disruption of Transcriptionally Active Stat3 Dimers with Non‐phosphorylated, Salicylic Acid‐Based Small Molecules: Potent in vitro and Tumor Cell Activities

Abstract

Three's company: A library of analogues of the previously reported Stat3 inhibitor S3I-201 was prepared. The most active analogues, SF-1-066 (X=NCH3) and SF-1-121 (X=O), have shown impressive in vitro and whole-cell activities that possibly result from the successful occupation of a third, hydrophobic subpocket of the Stat3 SH2 domain.