Selective noncovalent proteasome inhibiting activity of trifluoromethyl‐containing<i>gem</i>‐quaternary aziridines

Ielo, Laura; Patamia, Vincenzo; Citarella, Andrea; Schirmeister, Tanja; Stagno, Claudio; Rescifina, Antonio; Micale, Nicola; Pace, Vittorio

doi:10.1002/ardp.202300174

Cited by 3 publications

(1 citation statement)

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“…The ubiquitin-proteasome system is responsible for the maintenance of protein homeostasis and the regulation of various cellular processes. Proteasome inhibition is a strategy employed in the anti-cancer therapy ( Ielo et al, 2022 ; Ielo et al, 2023 ). Sosič and co-workers reported a series of coumarin derivatives as selective (immuno)proteasome inhibitors ( Schiffrer et al, 2021 ).…”

Section: Biological Applications Of Coumarin Derivativesmentioning

confidence: 99%

Syntheses, reactivity, and biological applications of coumarins

Citarella,

Vittorio,

Dank

et al. 2024

Front. Chem.

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This comprehensive review, covering 2021–2023, explores the multifaceted chemical and pharmacological potential of coumarins, emphasizing their significance as versatile natural derivatives in medicinal chemistry. The synthesis and functionalization of coumarins have advanced with innovative strategies. This enabled the incorporation of diverse functional fragments or the construction of supplementary cyclic architectures, thereby the biological and physico-chemical properties of the compounds obtained were enhanced. The unique chemical structure of coumarine facilitates binding to various targets through hydrophobic interactions pi-stacking, hydrogen bonding, and dipole-dipole interactions. Therefore, this important scaffold exhibits promising applications in uncountable fields of medicinal chemistry (e.g., neurodegenerative diseases, cancer, inflammation).

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Section: Biological Applications Of Coumarin Derivativesmentioning

confidence: 99%

Syntheses, reactivity, and biological applications of coumarins

Citarella,

Vittorio,

Dank

et al. 2024

Front. Chem.

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γ‐Cyclodextrins as Supramolecular Reactors for the Three‐component Aza‐Darzens Reaction in Water

Patamia,

Saccullo,

Zagni

et al. 2024

Chemistry A European J

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In recent decades, many efforts have been devoted to studying reactions catalyzed in nanoconfined spaces. The most impressive aspect of catalysis in nanoconfined spaces is that the reactivity of the molecules can be smartly driven to disobey classical behavior. A green and efficient three‐component aza‐Darzens (TCAD) reaction using a catalytic amount of g‐cyclodextrins (CDs) in water has been developed to synthesize N‐phenylaziridines. CDs effectively performed this reaction in an environmentally friendly setting, achieving good yields. The same reaction was then performed using polymeric g‐CD such as a g‐cyclodextrin polymer crosslinked (GCDPC) with epichlorohydrin, a sponge‐like macroporous g‐cyclodextrin‐based cryogel (GCDC), and a g‐cyclodextrin‐based hydrogel (GCDH). The homogeneous and heterogeneous catalyst recovery was then studied, and it was proved to be easily recycled several times without relevant activity loss. Water, as a unique and eco‐friendly reaction medium, has been utilized for the first time, to the best of our knowledge, in this reaction. The inclusion of the reagents in CDs has been studied and rationalized by NMR spectroscopy experiments and molecular modeling calculations. The credit of the presented protocol includes good yields and catalyst reusability and precludes the use of organic solvents.

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Organic contaminants in the groundwater of the Kerio Valley water basin, Baringo County, Kenya

Langat,

Kibet,

Okanga

et al. 2023

Eur J Chem

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Currently, groundwater is largely becoming the main source of fresh water in most developing countries. However, various deleterious impacts resulting from anthropogenic activities beneath the earth’s surface have significantly affected groundwater quality, as evidenced in several areas endowed with mineral and hydrocarbon deposits, agricultural activities, and industrial processes. The possible etiological impacts may include cancer and genetic aberrations which result from the toxic effects of organic waterborne contaminants ingested by humans and animals over time. The motivation behind this study was to identify and determine the concentration profiles of various organic pollutants in the wells located along the Kerio Valley water basin near the exploratory wells for hydrocarbons and mining activities. Therefore, this study is necessary in unraveling the level of organic contaminants in the sampled borehole water, which can then be extrapolated to cover other boreholes within the Kerio Valley basin. The study was carried out during the dry season of December 2022. The water samples from the boreholes were extracted using a solid phase extraction procedure and characterized using a gas chromatograph interfaced with a mass selective detector. The findings indicate that benzene derivatives which were mainly xylenes, 1,3,5-trimethylbenzene, 1-ethyl-3-methylbenzene, 1-methyl-2-propylpentylbenzene and polycyclic aromatic hydrocarbons such as naphthalene, phenanthrene, fluoranthene, azulene, and pyrene were found in most of the boreholes sampled. Furthermore, long-chain hydrocarbons were present in all groundwater samples with varying concentrations. The concentration of benzene derivatives ranged from 2.84 to 20.47 ppm. However, polycyclic hydrocarbons exhibited the highest concentrations of all organic pollutants, with pyrene giving a concentration of 23.14 ppm, fluoranthene (18.54 ppm), phenanthrene (14.13 ppm) and anthracene (11.06 ppm). According to the findings reported in this study, most of the borehole water in the Kerio Valley basin is contaminated and may be unsafe for drinking. Most of the reported concentration levels were several times higher than the standards of the U.S. Environmental and Protection Agency. However, it is necessary to develop a policy framework on the assessment and monitoring of water quality in the region and propose urgent measures to ensure a clean water supply for the benefit of residents.

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Selective noncovalent proteasome inhibiting activity of trifluoromethyl‐containinggem‐quaternary aziridines

Cited by 3 publications

References 51 publications

Syntheses, reactivity, and biological applications of coumarins

Syntheses, reactivity, and biological applications of coumarins

γ‐Cyclodextrins as Supramolecular Reactors for the Three‐component Aza‐Darzens Reaction in Water

Organic contaminants in the groundwater of the Kerio Valley water basin, Baringo County, Kenya

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