Revisiting the anticancer properties of phosphane(9-ribosylpurine-6-thiolato)gold(I) complexes and their 9H-purine precursors.

ABSTRACT: New mono- and di-nuclear thio-purine and thio-purine nucleoside gold(I) complexes were synthesized, characterized, and evaluated in vitro for biological activities in comparison to related known purine complexes. By combining known anti-tumoral thio-purines with R₃PAu moieties as present in auranofin, complexes with enhanced effects and selectivities were obtained, which not only act as cytostatics, but also disrupt tumor-specific processes. Their IC₅₀ values in cytotoxicity test with tumor cell lines ranged from three-digit nanomolar to single-digit micromolar, revealing a tentative structure-activity relationship (SAR). Both the residues R² of the phosphane ligand and R¹ at C2 of the pyrimidine ring had a significant impact on the cytotoxicity.

SUBMITTER: Kober L 

PROVIDER: S-EPMC9653339 | biostudies-literature | 2022 Dec

REPOSITORIES: biostudies-literature