Original ArticleAn anti-prostate cancer benzofuran-conjugated iridium(III) complex as a dual inhibitor of STAT3 and NF-κB

- Four benzofuran-conjugated metal complexes were synthesized and screened.
- Complex 1 was identified as the STAT3 and NF-κB dual inhibitor.
- Complex 1 engages and stabilizes STAT3 and NF-κB in cell lysates.
- Complex 1 shows the antiproliferative activity in the prostate cell line.

Four benzofuran-conjugated iridium(III) or rhodium (III)-based metal complexes are synthesized to screen as an inhibitor of STAT3 activity in prostate cancer cells. All complexes show the high stability and solubility in the biological system. In this study, an iridium(III) complex engages STAT3 and NF-κB to inhibit their translocation and transcriptional activities. Moreover, complex 1 shows more potential antiproliferative activity against DU145 cells and suppresses tumor growth in a prostate cancer xenograft mouse without observable adverse effects. Complex 1 may provide the basis for developing new therapeutic strategy in vivo and in vitro for the treatment of advanced prostate cancer.