Two novel Pd thiosemicarbazone complexes as efficient and selective antitumoral drugs

Abstract

Cancer is a leading cause of death worldwide, accounting for nearly 10 million deaths in 2020. Palladium complexes can be used as anticancer and pharmacological agents as a promising alternative...

Proving the Antimicrobial Therapeutic Activity on a New Copper–Thiosemicarbazone Complex

“…On the other hand, when they interact with cell culture media (e.g., serum, antibiotics), Cu­(HL) 2 seemed to partially stabilize the size maintaining the nanometric range in a fresh solution, which slightly reach some aggregation after longer contact times (52 vs 125 nm). In both horc cases, the protein corona formation was also confirmed by the ζ-potential shift from a negative charge in aqueous solution to more neutral values at both incubation times. A more neutral surface could explain the aggregation, observing similar colloidal performances in recently reported TSCN-based Pd complexes …”

“…), where the presence of diverse biological components (e.g., proteins, salts, electrolytes) could impact the complex solubility and/or charge, which could compromise their performances. In some cases, the solvent can cause inactivation − or the production of new species, which may affect its efficiency. , Hence, the identification of active species or the investigation of the physicochemical features under relevant environments (mainly structural and colloidal stability) has become a mandatory study for the evaluation of potential therapeutically active drugs. In order to shed light on its biological activity and suitability for the desired antimicrobial purposes, the stability profile of the Cu­(HL) 2 complex was monitored in diverse physiological media up to 24 h, starting from the simplest, such as aqueous solution (containing 1% of DMSO) or Tris-HCl/DMSO, to more complex ones, such as culture media (cellular or bacterial nutrient broth, NB), by using UV–visible spectroscopy for the structural stability (see Section and 3.2) or dynamic light scattering (DLS) for the colloidal stability (Section and Table S1).…”

“…A more neutral surface could explain the aggregation, observing similar colloidal performances in recently reported TSCN-based Pd complexes. 18 In terms of structural stability of metal complexes acting as potential drugs, a broadly applicable protein model for evaluating metallodrug−protein interactions (the hen egg white lysozyme (HEWL) by UV−vis, electrospray ionization (ESI) mass spectrometry, or X-ray) 41−43 is available. Highly positively charged with hydrophobic residues, HEWL is known as a suitable protein model for biological active binding examination, 44 giving insights into potential aggregation processes in body fluids.…”

“…In view of the above, the actual social needs, and our previous experience producing effective anticancer complexes using TSCN by a groove-binding model, we propose here an innovative antimicrobial copper therapeutic agent based on a similar TSCN with N4 substitution, H 2 L (N1-(4-(dimethylamino)­benzylidene)-N4-(4-nitrofenil)­thiosemicarbazone, Figure ). In this respect, the antibacterial efficacy of this Cu­(HL) 2 complex is evaluated using two diverse strains, widely recognized as appellant human pathogenic models with broadly propagation features: (i) Escherichia coli (E.…”

Michael addition-driven synthesis of cytotoxic palladium(ii) complexes from chromone thiosemicarbazones: investigation of anticancer activity throughin vitroandin vivostudies

“…Thiosemicarbazones (TSCs) (4CQN-NH-C(S)-No), an imperative class of Schiff base ligands, have received considerable attention due to their ability to form chelates with metal ions since mixed hard/soft (oxygen/nitrogen-sulfur) donor atoms could be involved in the coordination. [7][8][9][10] In most cases, chelation of these ligands to metal ions increased the inhibition of biosynthesis of DNA by blocking the enzyme ribonucleotide diphosphate reductase, inhibiting topoisomerase II activity, hindering base replication, creating lesions in DNA strands by oxidative rupture or binding to the nitrogen bases of DNA. [11][12][13] Several synthetic TSC derivatives and their transition metal complexes have been established in the literature with extensive medicinal properties.…”