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

作者：Hockey Samantha C; Barbante Gregory J; Francis Paul S; Altimari Jarrad M; Yoganantharajah Prusothman; Gibert Yann; Henderson Luke C^*

来源：European Journal of Medicinal Chemistry, 2016, 109: 305-313.

DOI：10.1016/j.ejmech.2015.12.035

• Click chemistry
• Iridium
• Triazole
• Prostate cancer

A range of 1,4-substituted 2-pyridyl-N-phenyl triazoles were synthesised and evaluated for their anti proliferative 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 mu M), 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 mu M for LNCaP and 0.85-5.9 mu M 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.

• 出版日期2016-2-15
• 单位迪肯大学