Chalcogenides-incorporating carbonic anhydrase inhibitors concomitantly reverted oxaliplatin-induced neuropathy and enhanced antiproliferative action

Tanini, Damiano; Carradori, Simone; Capperucci, Antonella; Lupori, Lucrezia; Zara, Susi; Ferraroni, Marta; Ghelardini, Carla; Mannelli, Lorenzo Di Cesare; Micheli, Laura; Lucarini, Elena; Carta, Fabrizio; Angeli, Andrea

doi:10.1016/j.ejmech.2021.113793

Cited by 26 publications

(26 citation statements)

References 56 publications

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“…Typically, selenium compounds exert their cytotoxic effects by acting as pro-oxidants and, therefore, altering the tumour cellular redox homeostasis, also preventing metastasis formation with significant specificity and efficiency, alongside with reduced side effects. In this context, a number of novel organoselenium compounds have been recently synthesized and tested as potential chemotherapeutic agents [ 63 ].…”

Section: Cancermentioning

confidence: 99%

The Role of Selenium in Pathologies: An Updated Review

2022

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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.

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Section: Cancermentioning

confidence: 99%

The Role of Selenium in Pathologies: An Updated Review

2022

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“…At the same time, the structure of compound 35c complexed with hCAII has been solved at a resolution of 1.35 Å ( Figure 2(B) ). The benzenesulfonamide scaffold showed the same binding mode as mentioned above, with the hydrogen bond between the oxygen of the sulphonamide group and Thr199 stabilising the binding of the inhibitor as in the case of complex with SmCA as typically found for this class of inhibitors 24 . Several hydrophobic interactions were observed also in this complex for both aromatic ring with Val121 and Leu198 and the terminal portion of the tail with Ile91.…”

Section: Resultsmentioning

confidence: 63%

Development of Praziquantel sulphonamide derivatives as antischistosomal drugs

Angeli

Ferraroni

Carta

et al. 2022

Journal of Enzyme Inhibition and Medicinal Chemistry

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The almost empty armamentarium to treat schistosomiasis, a neglected parasitic disorder caused by trematode flatworms of the genus Schistosoma , except Praziquantel (PZQ), urged to find new alternatives to fight this infection. Carbonic Anhydrase from Schistosoma mansoni (SmCA) is a possible new target against this nematode. Here, we propose new PZQ derivatives bearing a primary sulphonamide group in order to obtain hybrid drugs. All compounds were evaluated for their inhibition profiles on both humans and Schistosoma CAs, X-ray crystal data of SmCA and hCA II in adduct with some inhibitors were obtained allowing the understanding of the main structural factors responsible of activity. The compounds showed in vitro inhibition of immature and adult S. mansoni , but further optimisation is required for improved activity.

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“…valuable selenium-containing carbonic anhydrases inhibitors 60 [79,80] and activators 61 [81] (Figure 2).…”

Section: Synthesis Of Selenium-containing Small Moleculesmentioning

confidence: 99%

Synthesis and Applications of Organic Selenols

Tanini

Capperucci

2021

Adv Synth Catal

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The synthesis and the study of organoselenium compounds have received much attention over the past decades. Selenium-containing organic molecules are widely used in organic synthesis, materials science, and medicinal chemistry. Selenium -and more specifically the amino acid selenocysteine, bearing a selenol (SeH) moiety -is present in at least 25 human protein families, whose biological functions have not been completely identified. Amongst the variety of organoselenium compounds, selenols are a versatile class of molecules easily undergoing a broad array of useful transformations. Because of the unique properties of the SeH group, selenol chemistry has important applications in chemical sciences, spanning from organic synthesis to materials chemistry and biology. This review summarises currently available methodologies for the synthesis of selenols and highlights applications of selenols in chemical sciences and biology. Conclusions and Outlook 5.1. Safety Measures

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Chalcogenides-incorporating carbonic anhydrase inhibitors concomitantly reverted oxaliplatin-induced neuropathy and enhanced antiproliferative action

Cited by 26 publications

References 56 publications

The Role of Selenium in Pathologies: An Updated Review

The Role of Selenium in Pathologies: An Updated Review

Development of Praziquantel sulphonamide derivatives as antischistosomal drugs

Synthesis and Applications of Organic Selenols

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