An Easy Synthetic Approach to Construct Some Ebselen Analogues and Benzo[<i>b</i>]selenophene Derivatives: Their Antioxidant and Cytotoxic Assessment

Elsherbini, Mohamed; Hamama, Wafaa S.; Zoorob, Hanafi H.

doi:10.1002/jhet.3199

Cited by 17 publications

(11 citation statements)

References 71 publications

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“…Hence this method gives an easy synthetic entrance towards benzoselenophenopyrazoles. [60,61] Finally, due to their intrinsic electron deficiency caused by the fused pyrazole moiety the performance of iodolopyrazolium triflates in XB-based halide abstractions was investigated. In the solvolysis of benzhydryl halides with acetonitrile as the benchmark reaction iodolium salts of type 15 showed the highest activity outperforming previous reported bidentate XB-donors.…”

Section: Resultsmentioning

confidence: 99%

Iodolopyrazolium Salts – Synthesis, Derivatizations and Applications

Boelke

Kuczmera

Caspers

et al. 2020

Preprint

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Section: Resultsmentioning

confidence: 99%

Iodolopyrazolium Salts – Synthesis, Derivatizations and Applications

Boelke

Kuczmera

Caspers

et al. 2020

Preprint

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“…Compounds 43 and 44 ( Figure 11 ) were reported the same year by Hamama et al; also in this case no selectivity was observed, the compounds being endowed with a low micromolar anti-proliferative activity measured in the MCF-7 cell line and in the normal human lung fibroblast cell line (WI-38) [ 124 ].…”

Section: Antiproliferative Activitiesmentioning

confidence: 95%

Ebselen and Analogues: Pharmacological Properties and Synthetic Strategies for Their Preparation

2021

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Ebselen is the leader of selenorganic compounds, and starting from its identification as mimetic of the key antioxidant enzyme glutathione peroxidase, several papers have appeared in literature claiming its biological activities. It was the subject of several clinical trials and it is currently in clinical evaluation for the treatment of COVID-19 patients. Given our interest in the synthesis and pharmacological evaluation of selenorganic derivatives with this review, we aimed to collect all the papers focused on the biological evaluation of ebselen and its close analogues, covering the timeline between 2016 and most of 2021. Our analysis evidences that, even if it lacks specificity when tested in vitro, being able to bind to every reactive cysteine, it proved to be always well tolerated in vivo, exerting no sign of toxicity whatever the administered doses. Besides, looking at the literature, we realized that no review article dealing with the synthetic approaches for the construction of the benzo[d][1,2]-selenazol-3(2H)-one scaffold is available; thus, a section of the present review article is completely devoted to this specific topic.

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“…6,7 Interactions of ebselen with biological enzymes extended the inhibitory effects to antiviruses and antitoxins, laying an important foundation for the treatment of diseases and the production of drugs. 8−12 What is particularly exciting is its resistance to Corona Virus Disease 2019 (COVID- 19), which has spread worldwide in the first half of 2020. It has been found that for COVID-19, ebselen is a very promising lead compound to antiviral agent.…”

Section: Introductionmentioning

confidence: 99%

Ebselen-Agents for Sensing, Imaging and Labeling: Facile and Full-Featured Application in Biochemical Analysis

Zhang

Lei

Wang

et al. 2021

ACS Appl. Bio Mater.

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Phenyl-1,2-benzoselenazol-3(2H)-one (ebselen) is a classical mimic of glutathione peroxidase (GPx). Thioredoxin interaction endows ebselen attractive biological functions, such as antioxidation and anti-infection, as well as versatile therapeutic usage. Accordingly, application of ebselen analogues in biosensing, chemical labeling, imaging analysis, disease pathology, drug development, clinical treatment, etc. have been widely developed, in which mercaptans, reactive oxygen species, reactive sulfur species, peptides, and proteins were involved. Herein, focusing on the application of ebselen-agents in biochemistry, we have made a systematic summary and comprehensive review. First, we summarized both the classical and the innovative methods for preparing ebselen-agents to present the synthetic strategies. Then we discussed the full functional applicability of ebselen analogues in three fields of biochemical analysis including the fluorescence sensing and bioimaging, derivatization for high throughput fluorescence analysis, and the labeling gents for proteomics. Finally, we discussed the current challenges and perspectives for ebselen-agents as analytical tools in biological research. By presenting the multifunctional applicability of ebselen, we hope this review could appeal researchers to design the ebselen-related biomaterials for biochemical analysis.

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An Easy Synthetic Approach to Construct Some Ebselen Analogues and Benzo[b]selenophene Derivatives: Their Antioxidant and Cytotoxic Assessment

Cited by 17 publications

References 71 publications

Iodolopyrazolium Salts – Synthesis, Derivatizations and Applications

Iodolopyrazolium Salts – Synthesis, Derivatizations and Applications

Ebselen and Analogues: Pharmacological Properties and Synthetic Strategies for Their Preparation

Ebselen-Agents for Sensing, Imaging and Labeling: Facile and Full-Featured Application in Biochemical Analysis

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