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Mono-axial functionalised octahedral diazido Pt(iv) complexes trans, trans, trans-[Pt(py) 2 (N 3 ) 2 (OR 1 )(OR 2 )] (OR 1 = OH and OR 2 = anticancer agent coumarin-3 carboxylate (cou, 2a ), pyruvate dehydrogenase kinase (PDK) inhibitors 4-phenylbutyrate (PhB, 2b ) or dichloroacetate (DCA, 2c )), and their di-axial functionalised analogues with OR 1 = DCA and OR 2 = cou ( 3a ), PhB ( 3b ), or DCA ( 3c ) have been synthesised and characterised, including the X-ray crystal structures of complexes 2a, 3a, 3b and 3c . These complexes exhibit dark stability and have the potential to generate cytotoxic Pt(ii) species and free radicals selectively in cancer cells when irradiated. Mono-functionalised complexes 2a-2c showed higher aqueous solubility and more negative reduction potentials. Mono- and di-functionalised complexes displayed higher photocytotoxicity with blue light (1 h, 465 nm, 4.8 mW cm -2 ) than the parent dihydroxido complex 1 (OR 1 = OR 2 = OH) in A2780 human ovarian (IC 50 0.9-2.9 μM for 2a-2c ; 0.11-0.39 μM for 3a-3c ) and A549 human lung cancer cells (5.4-7.8 μM for 2a-2c ; 1.2-2.6 μM for 3a-3c ) with satisfactory dark stability. Notably, no apparent dark cytotoxicity was observed in healthy lung MRC-5 fibroblasts for all complexes (IC 50 &gt; 20 μM). Significantly higher platinum cellular accumulation and photo-generated ROS levels were observed for the di-functionalised complexes compared with their mono-functionalised analogues when cancer cells were treated under the same concentrations.

Axial functionalisation of photoactive diazido platinum(iv) anticancer complexes