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

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

doi:10.1016/j.canlet.2017.03.016

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

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^*

^*Corresponding author for this work

Department of Chemistry

Research output: Contribution to journal › Journal article › peer-review

74 Citations (Scopus)

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.

Original language	English
Pages (from-to)	76-84
Number of pages	9
Journal	Cancer Letters
Volume	396
DOIs	https://doi.org/10.1016/j.canlet.2017.03.016
Publication status	Published - 28 Jun 2017

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

SDG 3 Good Health and Well-being

User-Defined Keywords

Benzofuran-conjugated iridium(III) complex
Dual inhibitors
NF-κB
Prostate cells
STAT3

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10.1016/j.canlet.2017.03.016

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title = "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.",

keywords = "Benzofuran-conjugated iridium(III) complex, Dual inhibitors, NF-κB, Prostate cells, STAT3",

author = "Kang, \{Tian Shu\} and Wanhe Wang and Zhong, \{Hai Jing\} and Dong, \{Zhen Zhen\} and Qi Huang and Mok, \{Simon Wing Fai\} and Leung, \{Chung Hang\} and Wong, \{Vincent Kam Wai\} and Ma, \{Dik Lung\}",

note = "Funding Information: This work is supported by Hong Kong Baptist University (FRG2/15-16/002), the Health and Medical Research Fund (HMRF/14130522), the Research Grants Council (HKBU/12301115, HKBU/204612 and HKBU/201913), the French National Research Agency/Research Grants Council Joint Research Scheme (A-HKBU201/12-Oligoswitch), the Natural Science Foundation of China (21575121), Guangdong Province Natural Science Foundation (2015A030313816), the Hong Kong Baptist University Century Club Sponsorship Scheme 2016, Interdisciplinary Research Matching Scheme (RC-IRMS/15-16/03), the Science and Technology Development Fund, Macao SAR (098/2014/A2) and the University of Macau (MYRG2015-00137-ICMS-QRCM, MYRG2016-00151-ICMS-QRCM and MRG044/LCH/2015/ICMS) and the National Natural Science Foundation of China (No. 21628502). Publisher copyright: {\textcopyright} 2017 Elsevier B.V. All rights reserved.",

year = "2017",

month = jun,

day = "28",

doi = "10.1016/j.canlet.2017.03.016",

language = "English",

volume = "396",

pages = "76--84",

journal = "Cancer Letters",

issn = "0304-3835",

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TY - JOUR

T1 - An anti-prostate cancer benzofuran-conjugated iridium(III) complex as a dual inhibitor of STAT3 and NF-κB

AU - Kang, Tian Shu

AU - Wang, Wanhe

AU - Zhong, Hai Jing

AU - Dong, Zhen Zhen

AU - Huang, Qi

AU - Mok, Simon Wing Fai

AU - Leung, Chung Hang

AU - Wong, Vincent Kam Wai

AU - Ma, Dik Lung

N1 - Funding Information: This work is supported by Hong Kong Baptist University (FRG2/15-16/002), the Health and Medical Research Fund (HMRF/14130522), the Research Grants Council (HKBU/12301115, HKBU/204612 and HKBU/201913), the French National Research Agency/Research Grants Council Joint Research Scheme (A-HKBU201/12-Oligoswitch), the Natural Science Foundation of China (21575121), Guangdong Province Natural Science Foundation (2015A030313816), the Hong Kong Baptist University Century Club Sponsorship Scheme 2016, Interdisciplinary Research Matching Scheme (RC-IRMS/15-16/03), the Science and Technology Development Fund, Macao SAR (098/2014/A2) and the University of Macau (MYRG2015-00137-ICMS-QRCM, MYRG2016-00151-ICMS-QRCM and MRG044/LCH/2015/ICMS) and the National Natural Science Foundation of China (No. 21628502). Publisher copyright: © 2017 Elsevier B.V. All rights reserved.

PY - 2017/6/28

Y1 - 2017/6/28

N2 - 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.

AB - 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.

KW - Benzofuran-conjugated iridium(III) complex

KW - Dual inhibitors

KW - NF-κB

KW - Prostate cells

KW - STAT3

UR - https://www.scopus.com/pages/publications/85016138486

U2 - 10.1016/j.canlet.2017.03.016

DO - 10.1016/j.canlet.2017.03.016

M3 - Journal article

C2 - 28323031

AN - SCOPUS:85016138486

SN - 0304-3835

VL - 396

SP - 76

EP - 84

JO - Cancer Letters

JF - Cancer Letters

ER -

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

Abstract

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