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A series of gold(I) complexes involving triphenylphosphine (PPh 3 ) and one  N -donor ligand derived from deprotonated mono- or disubstituted hypoxanthine (HL n ) of the general composition [Au(L n )(PPh 3 )] ( 1 – 9 ) is reported. The complexes were thoroughly characterized, including multinuclear high resolution NMR spectroscopy as well as single crystal X-ray analysis (for complexes  1  and  3 ). The complexes were screened for their  in   vitro  cytotoxicity against human cancer cell lines MCF7 (breast carcinoma), HOS (osteosarcoma) and THP-1 (monocytic leukaemia), which identified the complexes  4 – 6  as the most promising representatives, who antiproliferative activity was further tested against A549 (lung adenocarcinoma), G-361 (melanoma), HeLa (cervical cancer), A2780 (ovarian carcinoma), A2780R (ovarian carcinoma resistant to  cisplatin ), 22Rv1 (prostate cancer) cell lines. Complexes  4 – 6  showed a significantly higher  in   vitro  anticancer effect against the employed cancer cells, except for G-361, as compared with the commercially used anticancer drug  cisplatin , with IC 50  ≈ 1–30 µM. Anti-inflammatory activity was evaluated  in   vitro  by the assessment of the ability of the complexes to modulate secretion of the pro-inflammatory cytokines, i.e. tumour necrosis factor-α (TNF-α) and interleukin-1β (IL-1β), in the lipopolysaccharide-activated macrophage-like THP-1 cell model. The results of this study identified the complexes as auspicious anti-inflammatory agents with similar or better activity as compared with the clinically applied gold-based antiarthritic drug Auranofin. In an effort to explore the possible mechanisms responsible for the biological effect, the products of interactions of selected complexes with sulfur-containing biomolecules (L-cysteine and reduced glutathione) were studied by means of the mass-spectrometry study.

Gold(I)-Triphenylphosphine Complexes with Hypoxanthine-Derived Ligands: In Vitro Evaluations of Anticancer and Anti-Inflammatory Activities