Cytotoxicity profiling of choline chloride-based natural deep eutectic solvents.

This study aims to examine in detail for the first time the cytotoxic profile of twelve choline chloride-based deep eutectic solvents (NADES) against HT-29, Caco-2, MCF-7, and MRC-5 cell lines. All NADES systems were synthesized by microwave synthesis using choline chloride as a hydrogen bond acceptor (HBA) and selected sugars, alcohols, organic acids, and urea as hydrogen bond donors (HBD) with the addition of 20% water (w/w) to all systems. It was observed that the cytotoxic effect predominantly depended on the structure of HBD.

Synthesis, characterization, antitumor potential, and investigation of mechanism of action of copper(ii) complexes with acylpyruvates as ligands: interactions with biomolecules and kinetic study.

Considering the urgency of finding a cure for vicious diseases such as tumors, we have synthesized and characterized a small series of new copper(ii) complexes with biologically important ligands such as acylpyruvate. In addition to this, we used another four copper(ii) complexes, with ligands of the same type to examine the antitumor potential. The antitumor potential of the copper(ii) complexes was examined on three tumor cell lines and one normal human cell line using the MTT assay.

Iron salt-promoted oxidation of steroidal phenols by -chloroperbenzoic acid: a route to possible antitumor agents.

A new oxidant, containing -chloroperoxybenzoic acid (MCPBA) and an iron salt, was developed and used for oxidation of steroidal phenols to a quinol/epoxyquinol mixture. Reaction was optimized for estrone, by varying initiators (Fe-salts), reaction temperature, time and mode of MCPBA application. A series of five more substrates (17β-estradiol and its hydrophobized derivatives) was subjected to the optimized oxidation, providing corresponding -quinols and 4β,5β-epoxyquinols in good to moderate yields.

Chitosan nanobeads loaded with Biginelli hybrids as cell-selective toxicity systems with a homogeneous distribution of the cell cycle in cancer treatment.

Tetrahydropyrimidines are a class of azaheterocycles, also called Biginelli hybrids (obtained from the Biginelli reaction), that have attracted an enormous interest in the medicinal chemistry community in recent years, due to a broad biological activity, such as anticancer, antiviral, anti-inflammatory, antidiabetic, antituberculosis activities, According to SciFinder®, more than 70 000 different Biginelli-like compounds have been covered in publications. However, although the Biginelli reaction can yield a large number of compounds with a broad range of activities, none of them have been captured in a carrier. In this study, chitosan-based (Ch) nanoparticles (NPs) containing three different molecules (Biginelli hybrids) were developed and tested for the first time as simple and promising vehicles for anticancer Biginelli-based drugs.