Journal
CANCER LETTERS
Volume 396, Issue -, Pages 76-84Publisher
ELSEVIER IRELAND LTD
DOI: 10.1016/j.canlet.2017.03.016
Keywords
Benzofuran-conjugated iridium(III) complex; STAT3; NF-kappa B; Prostate cells; Dual inhibitors
Categories
Funding
- Hong Kong Baptist University [FRG2/15-16/002]
- Health and Medical Research Fund [HMRF/14130522]
- Research Grants Council [HKBU/12301115, HKBU/204612, HKBU/201913]
- French National Research Agency/Research Grants Council Joint Research Scheme [A-HKBU201/12-Oligoswitch]
- Natural Science Foundation of China [21575121]
- Guangdong Province Natural Science Foundation [2015A030313816]
- Hong Kong Baptist University Century Club Sponsorship Scheme
- Interdisciplinary Research Matching Scheme [RC-IRMS/15-16/03]
- Science and Technology Development Fund
- Macao SAR [098/2014/A2]
- University of Macau [MYRG2015-00137-ICMS-QRCM, MYRG2016-00151-ICMS-QRCM, MRG044/LCH/2015/ICMS]
- National Natural Science Foundation of China [21628502]
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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-kappa B 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. (C) 2017 Elsevier B.V. All rights reserved.
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