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

Abstract

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.

• Authors: Tian-Shu Kang, Wanhe Wang, Hai-Jing Zhong, Zhen-Zhen Dong, Qi Huang, Simon Wing Fai Mok, Chung-Hang Leung, Vincent Kam Wai Wong, Dik-Lung Ma
• Journal: Cancer letters (Cancer Lett) Vol. 396 Pg. 76-84 (06 28 2017) ISSN: 1872-7980 [Electronic] Ireland
• PMID: 28323031 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
• Copyright: Copyright © 2017 Elsevier B.V. All rights reserved.

Chemical References

• Benzofurans
• NF-kappa B
• STAT3 Transcription Factor
• STAT3 protein, human
• Iridium
• benzofuran

Topics

• Animals
• Benzofurans (chemistry, pharmacology)
• Cell Line, Tumor
• HEK293 Cells
• Humans
• Iridium (chemistry, pharmacology)
• Male
• Mice
• Mice, Inbred C57BL
• NF-kappa B (antagonists & inhibitors, metabolism)
• Prostatic Neoplasms (drug therapy, metabolism)
• Random Allocation
• STAT3 Transcription Factor (antagonists & inhibitors, metabolism)
• Xenograft Model Antitumor Assays