Selenium is an essential microelement required for a number of biological functions. Selenium—and more specifically the amino acid selenocysteine—is present in at least 25 human selenoproteins involved in a wide variety of essential biological functions, ranging from the regulation of reactive oxygen species (ROS) concentration to the biosynthesis of hormones. These processes also play a central role in preventing and modulating the clinical outcome of several diseases, including cancer, diabetes, Alzheimer’s disease, mental disorders, cardiovascular disorders, fertility impairments, inflammation, and infections (including SARS-CoV-2). Over the past years, a number of studies focusing on the relationship between selenium and such pathologies have been reported. Generally, an adequate selenium nutritional state—and in some cases selenium supplementation—have been related to improved prognostic outcome and reduced risk of developing several diseases. On the other hand, supra-nutritional levels might have adverse effects. The results of recent studies focusing on these topics are summarized and discussed in this review, with particular emphasis on advances achieved in the last decade.

A series of benzenesulfonamides bearing selenourea moieties was obtained considering the ureido-sulfonamide , in Phase I clinical trials as antitumor agent, as a lead molecule. All compounds showed interesting inhibition potencies against the physiologically relevant human (h) carbonic anhydrase (hCAs, EC 4.2.1.1) isoforms I, II, IV, and IX. The most flexible analogues in the series- showed low nanomolar inhibition constants against hCA I, II, and IX. We assessed selected compounds on the antioxidant properties and binding modes and evaluated human prostate (PC3), breast (MDA-MB-231), and colon-rectal (HT-29) cancer cell lines both in normoxic and hypoxic conditions.

Aryl selenols effectively inhibit carbonic anhydrase.

Treatment of epoxides with bis(trimethylsilyl)-selenide under strictly controlled conditions allows to isolate b-hydroxy selenols which evidence an unexpected stability, taking into account their known propensity to afford diselenides. Also thiiranes and aziridines lead to functionalized selenols bearing a thiol and a N-Ts-or N-Boc-protected amino moiety on b-position. These selenols were stable enough to react with different electrophiles. Ab-initio DF calculations on two suitable model systems, n-propyl selenol and bhydroxy derivative, allow to ascribe the observed low tendency to oxidation to noncovalent interactions between the selenol moiety and the ÀOH group.

The structural modification of the resveratrol scaffold is currently an active issue in the quest for more potent and versatile antioxidant derivatives for biomedical applications. Disclosed herein is an expedient and efficient entry to a novel class of resveratrol derivatives featuring an unprecedented 2-phenylbenzoselenophene skeleton. The new compounds were obtained in good yields by direct selenenylation of resveratrol with Se(0) and SO 2 Cl 2 in dry THF. Varying the [Se : SO 2 Cl 2 : resveratrol] ratio resulted in the formation of the parent benzoselenophene (1) and/or mono (2) and/or dichloro (3) benzoselenophene derivatives. All the benzoselenophene derivatives proved to be more efficient than resveratrol in the 2,2-diphenyl-1-picrylhydrazyl (DPPH) and ferric reducing/antioxidant power (FRAP) assays, with 1 showing an activity nearly comparable to that of Trolox. 1-3 also proved to be more efficient inhibitors than the parent resveratrol in kinetic experiments of styrene autoxidation. DFT calculations of the O-H bond dissociation enthalpy (BDE) revealed that the introduction of the Se-atom causes a significant decrease of the BDE of 3-OH and 5-OH, with just a small increase of the 4'-OH BDE. Compounds 1-3 showed no cytotoxicity at 5 μM concentrations on human keratinocyte (HaCaT) and intestinal (CaCo-2) cell lines.

An unprecedented carbonic anhydrase-mediated hydrolysis of selenolesters enables the release of selenolates, acting as potent CA inhibitors. A wide range of functionalised selenolesters, smoothly achieved from the corresponding selenols, are studied.

A new series of β-aminochalcogenides were designed and synthesized to identify new carbonic anhydrase activator (CAA) agents as novel tools for the management of several neurodegenerative and metabolic disorders which represent a clinical challenge without effective therapies available. Some β-aminoselenides and β-aminotellurides showed effective CA activating effects and a potent antioxidant activity. CAAs may have applications for memory therapy and CA deficiency syndromes.

The effect of eight potassium salts (KF, K 3 PO 4 , KOCN, K 2 CO 3 , KCl, K 2 SO 4 , KBr and 2 KI) on glycerol carbonate (GC) is studied through NMR, DSC, solubility and ATR-3 FTIR experiments. From the solubility data, the main thermodynamic functions of 4 solution and solvation are estimated, and the mean molal activity coefficients are 5 calculated. The results suggest that the capability of an anion to establish hydrogen 6 bonds with the solvent molecules (or behave as a base, as in the case of fluoride, 7 phosphate, cyanate and carbonate) is the most important structural feature that 8 determines its effects on the solvent structure. On the other hand potassium iodide 9 behaves in an anomalous way, due to the large polarizability of the anion that can 10 form non-electrostatic, van der Waals dispersive intermolecular interactions.