Poster Presentation Royal Australian Chemical Institute National Congress 2026

Synthesis and characterisation of binuclear gold-based drugs for the effective treatment of cancer (#516)

Arthur AH Hentschel 1 , Pooran PK Kumar 1 , Ruchika RO Ojha 1 , Suresh SB Bhargava 1 , Magdalena MP Plebanski 2
  1. RMIT, School of Science, CAMIC, Melbourne, Victoria, Australia
  2. RMIT, School of Science, CAVA Lab, Melbourne, Victoria, Australia

Cancer is a health issue worldwide. Gold-based drugs like Auranofin achieve high selectivity, and therefore, lower strain on healthy cells by targeting multiple enzymes and mechanisms overexpressed in cancerous cells. The anti-cancer properties and high activity of Auranofin are attributed to a simple phosphorous ligand featuring ethyl groups: -PEt3.[1] This crucial structural element can be applied to existing digold drugs, which utilise the more common phosphine-aryl ligands. An example is [ClAu(µ-2-C6F4-PPh2)(κ2-2-C6F4-PPh2)AuCl] 1, which contains dual active gold centres with oxidation state +I and +III, resulting in unique and better anti-cancer activity. This avoids developed resistances towards metal drugs and opens multiple mode of actions to inhibit cancer growth.[2] The complex above can be prepared by oxidising [Au2(µ-2-C6F4-PPh2)2] 2 with PhICl2 to [Au2Cl2(µ-2-C6F4-PPh2)2] 3. Heating of a solution of 3 in toluene results after disproportionation in 1.[3]

We theorise that the introduction of the Phosphorous-alkyl motif into digold complexes ([ClAu(µ-2-C6F4-PEt2)(κ2-2- C6F4-PEt2)AuCl] 4) will enhance their biological activity. Additionally, the synthesised complexes are wholly new and were fully characterised by single-crystal XRD, NMR spectroscopy and others.

 

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  3. [3] … Bennett, M. A.; Bhargava, S. K.; Mirzadeh, N.; Privér, S. H.; Wagler, J.; Willis, A. C. Synthesis and interconversions of digold(I), tetragold(I), digold(II), gold(I)–gold(III) and digold(III) complexes of fluorine-substituted aryl carbanions. Dalton Trans. 2009, (36), 7537-7551.