Tetrazolylidene-Stabilized Gold(I) Complexes: Synthesis and Evaluation of Anticancer Activity In Vitro
Year: 2026
Type: article
Abstract: High Resolution Image Download MS PowerPoint Slide The first comprehensive study of a series of seven mesoionic tetrazolylidene gold(I) chloride complexes ( 1 – 7 ) featuring a range of alkyl and aryl substituents (Me, t -Bu, iPr, Ph, Tol, Dipp, Mes) is reported. Three synthetic pathways enabling access to scarcely explored abnormal 1,3-disubstituted tetrazolium ligand precursors ( L 1 – L 7 ) have been established. All complexes are characterized by NMR spectroscopy, mass spectrometry, and elemental analysis, confirming their composition and purity. Single-crystal X-ray crystallography of six gold(I) complexes ( 1 – 6 ) reveals nearly linear coordination (176.49(11)–179.0(2)°) at the gold(I) center and a distinct geometric arrangement across the series. NMR stability studies with model nucleophiles L- cysteine (Cys) and glutathione (GSH) support the structural findings, demonstrating rapid and complete reaction of complexes 1 – 7 with thiols, as confirmed by 1 H NMR and ESI-MS. The antiproliferative activity of the obtained complexes ( 1 – 7 ) and selected precursors ( L 2, L 3, L 5, L 7 ) has been evaluated using MTT assays against human A2780 (ovarian) and A549 (lung) cancer cell lines, alongside noncancerous VERO E6 kidney cells for comparison. Most of the complexes display high selectivity indices (SI A2780 = 63.2–86.7) and potent antiproliferative effects in the low submicromolar range against A2780, outperforming cisplatin and matching the activity of auranofin. Overall, the results presented here demonstrate the potential of gold(I) tetrazolylidene-based complexes for medicinal applications.
Source: Inorganic Chemistry
Institution: Technical University of Munich
Language: English
Subfield: Oncology
Field: Medicine
Domain: Health Sciences
Open Access status: hybrid
Estimated APC paid: $4,500
OpenAlex ID: W7154454501