A comparison of novel organoiridium(III) complexes and their ligands as a potential treatment for prostate cancer

Hockey, Samantha C., Barbante, Gregory J., Francis, Paul S., Altimari, Jarrad M., Yoganantharajah, Prusothman, Gibert, Yann and Henderson, Luke C. 2016, A comparison of novel organoiridium(III) complexes and their ligands as a potential treatment for prostate cancer, European journal of medicinal chemistry, vol. 109, pp. 305-313, doi: 10.1016/j.ejmech.2015.12.035.

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Title A comparison of novel organoiridium(III) complexes and their ligands as a potential treatment for prostate cancer
Author(s) Hockey, Samantha C.
Barbante, Gregory J.
Francis, Paul S.ORCID iD for Francis, Paul S. orcid.org/0000-0003-4165-6922
Altimari, Jarrad M.
Yoganantharajah, Prusothman
Gibert, Yann
Henderson, Luke C.ORCID iD for Henderson, Luke C. orcid.org/0000-0002-4244-2056
Journal name European journal of medicinal chemistry
Volume number 109
Start page 305
End page 313
Total pages 9
Publisher Elsevier
Place of publication Amsterdam, The Netherlands
Publication date 2016-02-15
ISSN 1768-3254
Keyword(s) Click chemistry
Prostate cancer
Summary A range of 1,4-substituted 2-pyridyl-N-phenyl triazoles were synthesised and evaluated for their antiproliferative properties against lymph node cancer of the prostate (LNCaP) and bone metastasis of prostate cancer (PC-3) cells. Excellent-to-low IC50 values were determined (5.6-250 μM), and a representative group of 4 ligands were then complexed to iridium(III) giving highly luminescent species. Re-evaluation of these compounds against both cell lines was then undertaken and improved potency (up to 72-fold) was observed, giving IC50 values of 0.36-11 μM for LNCaP and 0.85-5.9 μM for PC-3. Preliminary screens for in vivo toxicity were conducted using a zebrafish model showing a wide range of induced toxicity depending of the compound evaluated. Apoptosis and Caspase-3 levels were also determined and showed no statistical difference between some of the treated specimens and the controls. This study may identify novel therapeutic agents for advanced stage of prostate cancer in humans.
Language eng
DOI 10.1016/j.ejmech.2015.12.035
Field of Research 030503 Organic Chemical Synthesis
030401 Biologically Active Molecules
030201 Bioinorganic Chemistry
0304 Medicinal And Biomolecular Chemistry
1115 Pharmacology And Pharmaceutical Sciences
0305 Organic Chemistry
Socio Economic Objective 970103 Expanding Knowledge in the Chemical Sciences
HERDC Research category C1 Refereed article in a scholarly journal
ERA Research output type C Journal article
Copyright notice ©2016, Elsevier
Persistent URL http://hdl.handle.net/10536/DRO/DU:30081052

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