Phosphanegold(I) dithiocarbamates, R3PAu[SC(=S)N( iPr)CH2CH2OH] for R = Ph, Cy and Et: Role of phosphane-bound R substituents upon in vitro cytotoxicity against MCF-7R breast cancer cells and cell death pathways

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Abstract

The synthesis and characterisation of R3PAu[S 2CN(iPr)CH2CH2OH], for R = Ph (1), Cy (2) and Et (3)4, is reported. Compounds 1-3 are cytotoxic against the doxorubicin-resistant breast cancer cell line, MCF-7R, with 1 exhibiting greater potency and cytotoxicity than either of doxorubicin and cisplatin. Based on human apoptosis PCR-array analysis, caspase activities, DNA fragmentation, cell apoptotic assays, intracellular reactive oxygen species (ROS) measurements and human topoisomerase I inhibition, induction of apoptosis by 1, and necrosis by 2 and 3, are demonstrated, by both extrinsic and intrinsic pathways. Compound 1 activates the p53 gene, 2 activates only the p73 gene, whereas 3 activates both the p53 and p73 genes. Compounds 1 and 3 activate NF-κB, and each inhibits topoisomerase I. © 2013 Elsevier Masson SAS. All rights reserved.

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Jamaludin, N. S., Goh, Z. J., Cheah, Y. K., Ang, K. P., Sim, J. H., Khoo, C. H., … Tiekink, E. R. T. (2013). Phosphanegold(I) dithiocarbamates, R3PAu[SC(=S)N( iPr)CH2CH2OH] for R = Ph, Cy and Et: Role of phosphane-bound R substituents upon in vitro cytotoxicity against MCF-7R breast cancer cells and cell death pathways. European Journal of Medicinal Chemistry, 67, 127–141. https://doi.org/10.1016/j.ejmech.2013.06.038

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