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Synthesis and anticancer evaluation of new disulfides incorporating naphthalimide moiety 含有萘二甲酰亚胺分子的新型二硫化物的合成与抗癌评估
IF 1.3 4区 化学 Q3 Chemistry Pub Date : 2024-03-03 DOI: 10.1080/10426507.2024.2323018
Lu Xu , Shuangyan He , Chunlan Chi , Caiwen Li , Peipei Cui , Hongying Wang , Baoquan Chen

A series of new disulfides incorporating naphthalimide moiety were designed, synthesized and biologically evaluated against three human cancer cell lines (MCF-7, SMMC-7721 and Hela). Most of target compounds exhibited some degrees of anticancer activities, and some compounds displayed better effects than reference drugs PX-12 and 5-FU against the tested three cancer cells. Especially, compound 7d showed the most potent antiproliferative activity against MCF-7 cell lines with IC50 value of 3.19 μM. Compound 8a displayed prominent anticancer property against SMMC-7721 cell lines with IC50 value of 1.84 μM. Compound 6c possessed the most effective proliferation inhibitory activity against Hela cell lines with IC50 value of 2.14 μM. In addition, cytotoxicity evaluation indicated that most of the compounds had weak cytotoxicity to L929 cell lines.

我们设计、合成了一系列含有萘二甲酰亚胺分子的新型二硫化物,并针对三种人类癌症细胞系(MCF-7、SMMC-7721 和 Hela)进行了生物评估。大多数靶...
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引用次数: 0
Synthesis and in vitro carbonic anhydrase and acetylcholinesterase inhibitory activities of novel hydrazide–hydrazone compounds containing 1,2,4-triazole ring 含 1,2,4-三唑环的新型酰肼化合物的合成及其体外碳酸酐酶和乙酰胆碱酯酶抑制活性
IF 1.3 4区 化学 Q3 Chemistry Pub Date : 2024-03-03 DOI: 10.1080/10426507.2024.2320672
Efe Doğukan Dincel , Ebru Didem Kuran , Beyza Onarer , Yusuf Fıstıkçı , İlhami Gülçin , Nuray Ulusoy-Güzeldemirci

In this work, 1,2,4-triazole derived hydrazide–hydrazones were synthesized with a five-step synthesis pathway. The novel derivatives were characterized by various analytical methods. Acetylcholinesterase (AChE), and human carbonic anhydrase (hCA) inhibitory qualifications of these thirteen original compounds (4, 5al) were also determined. The overall biological activity results were very interesting. The reported compounds were found to be very effective inhibitors of hCA I, hCA II, and AChE enzymes with IC50 values in the range of 17.33−77.00 nM for hCA I (Acetazolamide IC50: 62.80 nM), 13.07−46.20 nM for hCA II (Acetazolamide IC50: 57.75 nM) and 4.91−36.47 nM for AChE (Tacrine IC50: 28.88 nM). Within the new compounds, 5i displayed the best hCA I, hCA II and AChE inhibitory activities with IC50 values of 17.33 nM, 13.07 nM, and 4.91 nM, respectively.

本研究采用五步合成法合成了 1,2,4-三氮唑衍生的肼基-肼酮。这些新型衍生物通过各种分析方法进行了表征。乙酰胆碱...
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引用次数: 0
Spectroscopic constants and anharmonic force field of thiirane: a theoretical study 硫环的光谱常数和非谐波力场:理论研究
IF 1.3 4区 化学 Q3 Chemistry Pub Date : 2024-03-03 DOI: 10.1080/10426507.2024.2316794
Wei-Xiu Pang , Yun-Bin Sun , Jian-Jun Zhao , Mei-Shan Wang , Xiao-Min Song

The potential interstellar medium molecule, thiirane, has received considerable attention of experimental and theoretical studies in recent years. The anharmonic force field and spectroscopic constants of thiirane are calculated using CCSD(T) and B3LYP methods employing correlation consistent basis sets. Molecular structure, ground state rotational constants, quartic and sextic centrifugal distortion constants, and fundamental frequencies of thiirane are compared with the available experimental data. The B3LYP and CCSD(T) results can reproduce them well. The rotational parameters and vibrational wave numbers of isotopologues for thiirane are also determined using B3LYP method. The new data obtained in this study might be used to assist astronomical search for thiirane.

近年来,潜在的星际介质分子硫环已受到实验和理论研究的极大关注。该分子的非谐波力场和光谱常数与星际介质中的巯基...
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引用次数: 0
Towards the synthesis of new sequestring hexadentate bisphosphonic ligands for iron ion chelation 合成用于铁离子螯合的新型螯合六齿双膦配体
IF 1.3 4区 化学 Q3 Chemistry Pub Date : 2024-03-03 DOI: 10.1080/10426507.2024.2316787
Mouna Ouechtati , Christelle Kouame , Julia Deschamp , Thibaut Legigan , Soufiane Touil , Evelyne Migianu-Griffoni , Maelle Monteil , Marc Lecouvey

This work presents the design and the synthesis of precursors of hexadentate bisphosphonic ligands able to complex iron cation. This study describes coupling reaction between natural siderophore entity and bisphosphonic acids. These latter have properties of complexing heavy metals. These compounds were obtained from amidation reaction between a protected and activated bisphosphonic compound and serine trilactone. In the intermediate species, all the hydroxyl groups of phosphorus are esterified with ethyl group. The coupling method gave access to triserinelactone-bisphosphonate conjugates in good yields.

本研究介绍了能够络合铁阳离子的六价双膦配体前体的设计与合成。这项研究描述了天然苷元与铁阳离子之间的偶联反应。
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引用次数: 0
Synthesis and antibacterial properties of alkyl substituted sulfonium salt 烷基取代锍盐的合成与抗菌特性
IF 1.3 4区 化学 Q3 Chemistry Pub Date : 2024-03-03 DOI: 10.1080/10426507.2024.2323020
Jing Li , Xiaodong Zhou , Yue Lin , Bingling Liu , Wenyang Chen , Chengcai Liu

The development of new antibacterial agents is particularly important in the battle against pathogenic microorganisms. In this study, sulfonium ions were used as the structural core to synthesize alkyl-substituted ionic compounds as antibacterial agents. The antimicrobial activity of sulfonium ionic compounds against Escherichia coli and Staphylococcus aureus was analyzed by measurement of the minimum inhibitory concentration and minimum bactericidal concentration. The effects of sulfonium salts on cell membrane integrity and permeability were investigated by detecting the extracellular proteins leakage of E. coli and S. aureus upon contact treatment, and observing the bacteria’s ultrastructural changes with transmission electron microscopy. The results showed that all the sulfonium salts exhibited resistant activity. Sulfonium salt with alkyl chain length of 16 carbon presented the strongest resistance with MIC of 30 and 3.75 μmol/L, and MBC of 120 and 60 μmol/L against E. coli and S. aureus, respectively. After treatment with sulfonium salts, the permeability of the membrane of E. coli and S. aureus cells changed, and the exudation of extracellular proteins increased significantly. The transmission electron microscope showed that the surface of the bacteria had shrunk and the cell walls had burst. The group of sulfonium salt compounds can destroy the integrity of cell membrane and change membrane permeability to achieve antibacterial purposes.

在与病原微生物的斗争中,开发新型抗菌剂尤为重要。本研究以磺离子为结构核心,合成了一种...
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引用次数: 0
Three-component reaction between 2-hydroxymethyl-5-phenylamino-pyran-4-one and aromatic acyl chlorides with potassium selenocyanate: Synthesis of 2-aryl-6-hydroxymethyl-1-phenyl-4-selenoxo-1,4-dihydro-pyrano[3,2-d]pyrimidin-8-one 2-羟甲基-5-苯基氨基-吡喃-4-酮与芳酰氯与硒氰酸钾的三组分反应:2-芳基-6-羟甲基-1-苯基-4-硒氧-1,4-二氢吡喃[3,2-d]嘧啶-8-酮的合成
IF 1.3 4区 化学 Q3 Chemistry Pub Date : 2024-02-01 DOI: 10.1080/10426507.2023.2281499
Zahra Ayagh , Mohammad H. Mosslemin , Mohammad R. Nateghi , Alireza Hassanabadi

We report an efficient method for the synthesis of 2-aryl-6-hydroxymethyl-1-phenyl-4-selenoxo-1,4-dihydro-pyrano[3,2-d]pyrimidin-8-one from the condensation of potassium selenocyanate and aromatic acyl chlorides with 2-hydroxymethyl-5-phenylamino-pyran-4-one in the presence of catalytic amounts of N-methylimidazole under solvent-free conditions. This new protocol offers advantages such as mild reaction conditions, short reaction time, easy work-up, high yield products, and does not involve any hazardous solvent.

本文报道了一种由硒氰酸钾与芳香烃缩合合成2-芳基-6-羟甲基-1-苯基-4-硒氧基-1,4-二氢吡喃[3,2-d]嘧啶-8- 1的有效方法。
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引用次数: 0
Obtaining nano calcium fluoride and ammonium sulfate from phosphogypsum 从磷石膏中制备纳米氟化钙和硫酸铵
IF 1.3 4区 化学 Q3 Chemistry Pub Date : 2024-02-01 DOI: 10.1080/10426507.2023.2281475
Yassine Ennaciri , Mohammed Bettach , Hanan El Alaoui-Belghiti

This study presents an efficient and sustainable procedure for converting phosphogypsum (PG) waste, along with hydrofluoric acid (HF) and ammonia (NH3), into valuable materials. The results obtained demonstrate the high efficiency of this proposed procedure, resulting in the synthesis of relatively pure calcium fluoride (CaF2) nanoparticles and ammonium sulfate ((NH4)2SO4). The latter is recommended for agricultural use as a fertilizer, while the obtained CaF2 can be utilized in the metallurgical industry. Furthermore, this procedure not only offers a solution for reducing fluorine gas emissions and managing PG waste but also contributes to the conservation of fluorite reserves.

本研究提出了一种高效和可持续的方法,将磷石膏(PG)废物以及氢氟酸(HF)和氨(NH3)转化为有价值的材料。结果得到……
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引用次数: 0
The chemical behavior of the different impurities present in Phosphogypsum: a review 磷石膏中不同杂质的化学性质综述
IF 1.3 4区 化学 Q3 Chemistry Pub Date : 2024-02-01 DOI: 10.1080/10426507.2023.2281489
Yassine Ennaciri , Mohammed Bettach

Phosphogypsum (PG) is an acidic by-product that is created during the production of phosphoric acid using the sulfuric acid route. The management of PG poses a significant environmental challenge worldwide due to its large quantity and chemical composition. While PG primarily consists of calcium sulfate dihydrate, it also contains various impurities such as phosphorus, fluoride, heavy metals, and radionuclides. These toxic impurities, when present in high concentrations, can have adverse effects on the environment and human health. In this review, we provide a detailed examination of the behavior of the most abundant impurities found in PG. Furthermore, we discuss the factors that influence the presence of different types of impurities in PG. Understanding the overall behavior of these impurities is crucial for selecting appropriate environmental methods for PG management and identifying suitable avenues for its valorization.

磷石膏(PG)是一种酸性副产物,在使用硫酸路线生产磷酸过程中产生。PG的管理提出了一个重大的环境挑战。
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引用次数: 0
Synthesis, synthetic interests, and biological activities of β-substituted vinylphosphonates β-取代乙烯基膦酸盐的合成、合成兴趣和生物活性
IF 1.3 4区 化学 Q3 Chemistry Pub Date : 2024-02-01 DOI: 10.1080/10426507.2023.2281472
Cécile Garzon , Mireille Attolini , Michel Maffei

β-Substituted vinylphosphonates constitute an original class of organophosphorus reagents of which several compounds exhibit attractive biological properties. The review exemplifies and discusses the different synthetic methods described for their synthesis, which involve well known reactions, but also more specifically designed methods. In addition, the uses as synthetic intermediates as well as the therapeutic uses of the title compounds are also summarized.

β-取代的乙烯基膦酸盐构成了一类原始的有机磷试剂,其中一些化合物具有吸引人的生物学特性。这篇评论举例说明并讨论了……
{"title":"Synthesis, synthetic interests, and biological activities of β-substituted vinylphosphonates","authors":"Cécile Garzon ,&nbsp;Mireille Attolini ,&nbsp;Michel Maffei","doi":"10.1080/10426507.2023.2281472","DOIUrl":"10.1080/10426507.2023.2281472","url":null,"abstract":"<div><p>β-Substituted vinylphosphonates constitute an original class of organophosphorus reagents of which several compounds exhibit attractive biological properties. The review exemplifies and discusses the different synthetic methods described for their synthesis, which involve well known reactions, but also more specifically designed methods. In addition, the uses as synthetic intermediates as well as the therapeutic uses of the title compounds are also summarized.</p></div>","PeriodicalId":20056,"journal":{"name":"Phosphorus, Sulfur, and Silicon and the Related Elements","volume":null,"pages":null},"PeriodicalIF":1.3,"publicationDate":"2024-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138513447","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Rh(I)-catalyzed enantioselective (3 + 2) transannulations of 1,2,3-thiadiazoles with P-chiral monodentate phosphines Rh(I)催化1,2,3-噻二唑与p -手性单齿膦的对映选择性(3 + 2)转环反应
IF 1.3 4区 化学 Q3 Chemistry Pub Date : 2024-02-01 DOI: 10.1080/10426507.2023.2281473
Hao Wei , Cunzhi Chen , Aijun Gao , Zhanhui Yang

As a proof of concept, P-chiral monodentate phosphines, which were inactive in promoting the transannulations of 1,2,3-thiadiazoles, were proven viable in the asymmetric catalytic (3 + 2) transannulations of 1,2,3-thiadiazoles with a strained bicyclic alkene. Polycyclic dihydrothiophenes with four newly formed stereocenters are generated in moderate 19-72% yields and 11-27% enantiopurities.

作为概念的证明,p手性单齿膦在促进1,2,3-噻二唑的转环反应中没有活性,但在不对称催化(3 + 2)转环反应中是可行的。
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引用次数: 0
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Phosphorus, Sulfur, and Silicon and the Related Elements
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