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

European Journal of Medicinal Chemistry
Samantha C HockeyLuke C Henderson

Abstract

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.

References

Jun 30, 2010·Journal of Enzyme Inhibition and Medicinal Chemistry·Rajeev KharbMohammed Shahar Yar
Aug 2, 2011·Beilstein Journal of Organic Chemistry·Kumari ShaliniPramod Kumar Sharma
Sep 29, 2011·Chemistry, an Asian Journal·Sandip G AgalaveVandana S Pore
Jan 9, 2014·CA: a Cancer Journal for Clinicians·Rebecca SiegelAhmedin Jemal
May 16, 2014·Metallomics : Integrated Biometal Science·Vojtech NovohradskyViktor Brabec

❮ Previous
Next ❯

Citations

Dec 23, 2017·Dalton Transactions : an International Journal of Inorganic Chemistry·Quinn V C van HilstJames D Crowley
Aug 30, 2019·Dalton Transactions : an International Journal of Inorganic Chemistry·Roberto SoleJohannes G de Vries
Jun 25, 2017·European Journal of Medicinal Chemistry·Ze-Dong MouXia Zhang
Jul 18, 2020·Recent Patents on Anti-cancer Drug Discovery·Katerina I SlavovaIrena P Kostova
Jul 9, 2016·Journal of Inorganic Biochemistry·Benjamin J PagesJanice R Aldrich-Wright

❮ Previous
Next ❯

Related Concepts

Related Feeds

Apoptosis

Apoptosis is a specific process that leads to programmed cell death through the activation of an evolutionary conserved intracellular pathway leading to pathognomic cellular changes distinct from cellular necrosis