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Thiosemicarbazones continue to attract the interest of researchers as potential anticancer drugs. For example, 3-aminopyridine-2-carboxaldehyde thiosemicarbazone, or triapine, is the most well-known representative of this class of compounds that has entered multiple phase I and II clinical trials. Two new triapine derivatives HL 1  and HL 2  were prepared by condensation reactions of 2-pyridinamidrazone and S-methylisothiosemicarbazidium chloride with 3- N -( tert -butyloxycarbonyl) amino-pyridine-2-carboxaldehyde, followed by a Boc-deprotection procedure. Subsequent reaction of HL 1  and HL 2  with CuCl 2 ·2H 2 O in 1:1 molar ratio in methanol produced the complexes [Cu II (HL 1 )Cl 2 ]·H 2 O ( 1·H 2 O ) and [Cu II (HL 2 )Cl 2 ] ( 2 ). The reaction of HL 2  with Fe(NO 3 ) 3 ∙9H 2 O in 2:1 molar ratio in the presence of triethylamine afforded the complex [Fe III (L 2 ) 2 ]NO 3 ∙0.75H 2 O ( 3∙0.75H 2 O ), in which the isothiosemicarbazone acts as a tridentate monoanionic ligand. The crystal structures of HL 1  , HL 2  and metal complexes 1 and 2 were determined by single crystal X-ray diffraction. The UV-Vis and EPR spectroelectrochemical measurements revealed that complexes 1 and 2 underwent irreversible reduction of Cu(II) with subsequent ligand release, while 3 showed an almost reversible electrochemical reduction in dimethyl sulfoxide (DMSO). Aqueous solution behaviour of HL 1  and 1, as well as of HL 2  and its complex 2 , was monitored as well. Complexes 1 - 3 were tested against ovarian carcinoma cells, as well as noncancerous embryonic kidney cells, in comparison to respective free ligands, triapine and cisplatin. While the free ligands HL 1  and HL 2  were devoid of antiproliferative activity, their respective metal complexes showed remarkable antiproliferative activity in a micromolar concentration range. The activity was not related to the inhibition of ribonucleotide reductase (RNR) R2 protein, but rather to cancer cell homeostasis disturbance-leading to the disruption of cancer cell signalling.

Triapine Derivatives Act as Copper Delivery Vehicles to Induce Deadly Metal Overload in Cancer Cells