Ascorbate: a forgotten component in the cytotoxicity of Cu(II) ATCUN peptide complexes.

In 1983, Linus Pauling and colleagues reported about enhanced antitumor activity of the Cu(II) complex of the simplest ATCUN (amino terminal Cu(II) and Ni(II)-binding motif) peptide (NH-Gly-Gly-His-COOH, GGH) in the presence of ascorbate as an additive. In the following 4 decades, structural modifications of this complex were implemented, however, anticancer activity could not be significantly increased. This has led to neglecting the ATCUN motif and its Cu(II) complexes as potential chemotherapeutic agents.

Gold(III) complexes with thiosemicarbazone ligands: insights into their cytotoxic effects on lung cancer cells.

Cancer continues to pose a global threat, underscoring the urgent need for more effective and safer treatment options. Gold-based compounds have recently emerged as promising candidates due to their diverse range of biological activities. In this study, three gold(III) complexes derived from thiosemicarbazone ligands have been synthesized, fully characterized, including their X-ray crystal structures.

Bromo- and glycosyl-substituted BODIPYs for application in photodynamic therapy and imaging.

The introduction of heavy atoms into the BODIPY-core structure has proven to be a straightforward strategy for optimizing the design of such dyes towards enhanced generation of singlet oxygen rendering them suitable as photosensitizers for photodynamic therapy (PDT). In this work, BODIPYs are presented by combining the concept of bromination with nucleophilic aromatic substitution (SAr) of a pentafluorophenyl or a 4-fluoro-3-nitrophenyl moiety to introduce functional groups, thus improving the phototoxic effect of the BODIPYs as well as their solubility in the biological environment. The nucleophilic substitution enabled functionalization with various amines and alcohols as well as unprotected thiocarbohydrates.

Impact of N-heteroaromatic N-termini in Cu(II) ATCUN metallopeptides on their biorelevant redox activity.

Cu(II) complexes with ATCUN peptide ligands have been investigated for their ROS (reactive oxygen species) generation and oxidative DNA degradation abilities. The biological activity of most ATCUN complexes such as Cu-GGH (Gly-Gly-His) is, however, low. Tuning the redox chemistry by incorporation of N-heteroaromatics reinstates ROS production which leads to efficient DNA cleavage.