: In addition to providing a succinct pathway for the stereoselective synthesis of dapoxetine, a potent SSRI employed in the treatment of premature ejaculation, this study highlights the strategic use of Ellman's sulfinamide as a chiral auxiliary. The key method involves the diastereoselective allylation of (S,E)-N-Benzylidenesulfinamide, resulting in the desired S-configuration critical for the pharmacological activity of dapoxetine. The utilization of readily available benzaldehyde as the starting material and 1-naphthol as a late-stage coupling partner contributes to the economic feasibility of the synthesis. Especially, the linear synthetic approach adopted in this study employs simplified and more efficient protocols for various transformations, culminating in an overall yield of 26%. This research not only presents a practical synthetic route for dapoxetine, but also underscores the importance of cost-effective and streamlined methodologies in drug development processes.
:这项研究除了提供了立体选择性合成达泊西汀（一种用于治疗早泄的强效 SSRI）的简洁途径外，还强调了埃尔曼亚磺酰胺作为手性助剂的战略用途。关键方法包括对(S,E)-N-苄基亚磺酰胺进行非对映选择性烯丙基化，从而获得对达泊西汀药理活性至关重要的所需 S 构型。利用现成的苯甲醛作为起始原料，1-萘酚作为后期偶联剂，有助于提高合成的经济可行性。特别是，本研究采用的线性合成方法简化了各种转化过程，提高了转化效率，最终总产率达到 26%。这项研究不仅提出了一条实用的达泊西汀合成路线，还强调了药物开发过程中成本效益和简化方法的重要性。
{"title":"A Linear and Stereoselective Approach for the Synthesis of Dapoxetine from Benzaldehyde","authors":"Ramakoteswara Rao Chinta, Kumaraswamy Paridala, Vijay Kumar Tulam","doi":"10.2174/0115701786288732240214102952","DOIUrl":"https://doi.org/10.2174/0115701786288732240214102952","url":null,"abstract":": In addition to providing a succinct pathway for the stereoselective synthesis of dapoxetine, a potent SSRI employed in the treatment of premature ejaculation, this study highlights the strategic use of Ellman's sulfinamide as a chiral auxiliary. The key method involves the diastereoselective allylation of (S,E)-N-Benzylidenesulfinamide, resulting in the desired S-configuration critical for the pharmacological activity of dapoxetine. The utilization of readily available benzaldehyde as the starting material and 1-naphthol as a late-stage coupling partner contributes to the economic feasibility of the synthesis. Especially, the linear synthetic approach adopted in this study employs simplified and more efficient protocols for various transformations, culminating in an overall yield of 26%. This research not only presents a practical synthetic route for dapoxetine, but also underscores the importance of cost-effective and streamlined methodologies in drug development processes.","PeriodicalId":18116,"journal":{"name":"Letters in Organic Chemistry","volume":null,"pages":null},"PeriodicalIF":0.8,"publicationDate":"2024-02-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139956556","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}
: Clofarabine (1) is an anticancer agent used to treat acute leukemia. This work discloses the efforts to develop a convenient, environmentally benign, and high-yielding synthetic protocol leading to Clofarabine (1). The synthesis includes bromination of 2-deoxy-2-β-fluoro-1,3,5-tri-O-benzoyl-1- α-D-ribofuranose (6), followed by C-N coupling with a 2,6-dichloro purine (4) and selective amination consecutively. The proposed total synthesis comprises five steps to afford an overall yield of 65- 70% with 99.85% purity. The present process provides preparation of Clofarabine (1) using a simple purification process with lesser reaction time, better yield, and purity without using toxic and pyrophoric chemicals.
{"title":"A Simple and Efficient Path for the Synthesis Antineoplastic Agent (2R,3R,4S,5R)-5-(6-Amino-2-Chloropurin-9-yl)-4-Fluoro-2-(Hydroxymethyl) oxolan-3-ol (Clofarabine)","authors":"Laxmi Kumari Nagarapu, Chithaluri Sudhakar, Suresh Babu Namani","doi":"10.2174/0115701786287468240209105224","DOIUrl":"https://doi.org/10.2174/0115701786287468240209105224","url":null,"abstract":": Clofarabine (1) is an anticancer agent used to treat acute leukemia. This work discloses the efforts to develop a convenient, environmentally benign, and high-yielding synthetic protocol leading to Clofarabine (1). The synthesis includes bromination of 2-deoxy-2-β-fluoro-1,3,5-tri-O-benzoyl-1- α-D-ribofuranose (6), followed by C-N coupling with a 2,6-dichloro purine (4) and selective amination consecutively. The proposed total synthesis comprises five steps to afford an overall yield of 65- 70% with 99.85% purity. The present process provides preparation of Clofarabine (1) using a simple purification process with lesser reaction time, better yield, and purity without using toxic and pyrophoric chemicals.","PeriodicalId":18116,"journal":{"name":"Letters in Organic Chemistry","volume":null,"pages":null},"PeriodicalIF":0.8,"publicationDate":"2024-02-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139950393","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}
:: A variety of dihydropyrimidone compounds were synthesised using an effective one-pot, multicomponent, environmentally friendly reaction of aromatic aldehydes, urea/thiourea, ethyl acetoacetate, and glycerol/ethyl lactate. To the best of our knowledge, this is the first catalyst-free strategy for the synthesis of this key scaffold with medicinal chemistry applications. Other significant aspects of the current approach consist of the employment of glycerol/ethyl lactate as a biodegradable and environmentally friendly reaction medium-cum-promoter, the use of easily available substrates, moderate reaction conditions, ease of use, a wide substrate scope, a short reaction time, easy workup, and excellent yields, and atom efficiency, which make the disclosed procedure an excellent alternative to existing methods.
{"title":"Catalyst-free Approach to Dihydropyrimidones Using Glycerol/Ethyl Lactate as a Recyclable and Biodegradable Promoting Medium","authors":"Smriti Kushwaha, Swastika Singh, Jyoti Baranwal, Archana Jyoti","doi":"10.2174/0115701786277258231218092916","DOIUrl":"https://doi.org/10.2174/0115701786277258231218092916","url":null,"abstract":":: A variety of dihydropyrimidone compounds were synthesised using an effective one-pot, multicomponent, environmentally friendly reaction of aromatic aldehydes, urea/thiourea, ethyl acetoacetate, and glycerol/ethyl lactate. To the best of our knowledge, this is the first catalyst-free strategy for the synthesis of this key scaffold with medicinal chemistry applications. Other significant aspects of the current approach consist of the employment of glycerol/ethyl lactate as a biodegradable and environmentally friendly reaction medium-cum-promoter, the use of easily available substrates, moderate reaction conditions, ease of use, a wide substrate scope, a short reaction time, easy workup, and excellent yields, and atom efficiency, which make the disclosed procedure an excellent alternative to existing methods.","PeriodicalId":18116,"journal":{"name":"Letters in Organic Chemistry","volume":null,"pages":null},"PeriodicalIF":0.8,"publicationDate":"2024-02-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139760849","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}
Pub Date : 2024-02-02DOI: 10.2174/0115701786283444231128061732
Sibel Demir Kanmazalp, Necmi Dege, Nabajyoti Baildya, Suman Adhikari
: In the carbamate Schiff base compound, the molecule is stabilized by intramolecular hydrogen bonding interactions along with π···π stacking and C–H···π contacts that lead to the molecule generating diverse supramolecular architecture. The fingerprint plots associated with Hirshfeld surface analysis indicate that the most important contributions for the crystal packing are from H⋯H/H⋯H (81.8%), H⋯O/O⋯H (7.5%), and H⋯N/N⋯H (1.9%) interactions. Furthermore, a computational study is performed to find the interaction energy between molecular pairs, and a description of the active site of the compound has been included. The study inferred the role of various types of interaction energies in stabilizing the molecular pair. Additionally, the carbamate Schiff base compound was tested as a possible inhibitor for a group of the SARS-CoV-2 proteins employing a molecular docking approach. Papain-like protease (PLpro) was shown to have the highest binding affinities. The carbamate Schiff base compound with PLpro’s docking score falls within the acceptable levels for a hit compound.
{"title":"Exploring the Supramolecular Features, Computational Studies, and Molecular Docking Studies of a Carbamate Schiff Base","authors":"Sibel Demir Kanmazalp, Necmi Dege, Nabajyoti Baildya, Suman Adhikari","doi":"10.2174/0115701786283444231128061732","DOIUrl":"https://doi.org/10.2174/0115701786283444231128061732","url":null,"abstract":": In the carbamate Schiff base compound, the molecule is stabilized by intramolecular hydrogen bonding interactions along with π···π stacking and C–H···π contacts that lead to the molecule generating diverse supramolecular architecture. The fingerprint plots associated with Hirshfeld surface analysis indicate that the most important contributions for the crystal packing are from H⋯H/H⋯H (81.8%), H⋯O/O⋯H (7.5%), and H⋯N/N⋯H (1.9%) interactions. Furthermore, a computational study is performed to find the interaction energy between molecular pairs, and a description of the active site of the compound has been included. The study inferred the role of various types of interaction energies in stabilizing the molecular pair. Additionally, the carbamate Schiff base compound was tested as a possible inhibitor for a group of the SARS-CoV-2 proteins employing a molecular docking approach. Papain-like protease (PLpro) was shown to have the highest binding affinities. The carbamate Schiff base compound with PLpro’s docking score falls within the acceptable levels for a hit compound.","PeriodicalId":18116,"journal":{"name":"Letters in Organic Chemistry","volume":null,"pages":null},"PeriodicalIF":0.8,"publicationDate":"2024-02-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139664715","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}
: An efficient approach for the tosyloxyl group transfer in several N-arylbenzamides has been achieved using HTIB (Koser’s reagent) under mild reaction conditions. Its simplicity, efficiency, and reduced reliance on hazardous reagents make it an attractive choice for chemists seeking sustainable alternatives. The proposed methodology offered single-step para-selective tosyloxylation, ensuring the prevention of the synthesis of mixtures of ortho and meta-isomers. The corresponding products were obtained with moderate to excellent efficiency. The current approach eliminated the need for harsh, acidic, and toxic metals, ensuring safer handling and minimizing environmental impact. A plausible mechanism for tosyloxylation of N-arylbenzamides involving iodonium ylide has been proposed.
{"title":"Metal-Free Selective para-Tosyloxylation of N-Arylbenzamides using [Hydroxy( tosyloxy)iodo]benzene","authors":"Neha Rani, Deepak Kumar Aneja, Mayank Kinger, Rinku Soni, Monika Sihag, Sandeep Malik","doi":"10.2174/0115701786275866231117113843","DOIUrl":"https://doi.org/10.2174/0115701786275866231117113843","url":null,"abstract":": An efficient approach for the tosyloxyl group transfer in several N-arylbenzamides has been achieved using HTIB (Koser’s reagent) under mild reaction conditions. Its simplicity, efficiency, and reduced reliance on hazardous reagents make it an attractive choice for chemists seeking sustainable alternatives. The proposed methodology offered single-step para-selective tosyloxylation, ensuring the prevention of the synthesis of mixtures of ortho and meta-isomers. The corresponding products were obtained with moderate to excellent efficiency. The current approach eliminated the need for harsh, acidic, and toxic metals, ensuring safer handling and minimizing environmental impact. A plausible mechanism for tosyloxylation of N-arylbenzamides involving iodonium ylide has been proposed.","PeriodicalId":18116,"journal":{"name":"Letters in Organic Chemistry","volume":null,"pages":null},"PeriodicalIF":0.8,"publicationDate":"2024-02-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139664592","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}
Herein, we present a mild and effective synthetic method for preparing para-substituted 2-hydroxymethyl piperazine from serine methyl ester and L-amino acids with residues of different sizes. This synthetic route has several advantages including mild reaction conditions, availability of reagents, non-racemic composition, and the potential for gram-scale synthesis. Notably, the compound (4g) demonstrated excellent yields in our experiments.
{"title":"Mild and efficient synthesis of para-substituted 2-hydroxymethyl piperazine....","authors":"Zijian Liang, Liyuan Guo, Qian Li, Chunyan Liu, Chao Liu, Shi Wu","doi":"10.2174/0115701786283816240123103232","DOIUrl":"https://doi.org/10.2174/0115701786283816240123103232","url":null,"abstract":"Herein, we present a mild and effective synthetic method for preparing para-substituted 2-hydroxymethyl piperazine from serine methyl ester and L-amino acids with residues of different sizes. This synthetic route has several advantages including mild reaction conditions, availability of reagents, non-racemic composition, and the potential for gram-scale synthesis. Notably, the compound (4g) demonstrated excellent yields in our experiments.","PeriodicalId":18116,"journal":{"name":"Letters in Organic Chemistry","volume":null,"pages":null},"PeriodicalIF":0.8,"publicationDate":"2024-02-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139664668","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}
: Computational modeling has become a crucial tool in drug design, offering efficiency and cost-effectiveness. This paper discusses the various computational modeling techniques used in drug design and their role in enabling efficient drug discovery strategies. Molecular docking predicts the binding affinity of a small molecule to a target protein, allowing the researchers to identify potential lead compounds and optimize their interactions. Molecular dynamics simulations provide insights into protein-ligand complexes, enabling the exploration of conformational changes, binding free energies, and fundamental protein-ligand interactions. Integrating computational modeling with machine learning algorithms, such as QSAR modeling and virtual screening, enables the prediction of compound properties and prioritizes potential drug candidates. High-performance computing resources and advanced algorithms are essential for accelerating drug design workflows, with parallel computing, cloud computing, and GPU acceleration reducing computational time. The paper also addresses the challenges and limitations of computational modeling in drug design, such as the accuracy of scoring functions, protein flexibility representation, and validation of predictive models. It emphasizes the need for experimental validation and iterative refinement of computational predictions to ensure the reliability and efficacy of designed drugs.
{"title":"Harnessing Computational Modeling for Efficient Drug Design Strategies","authors":"Kuldeep Singh, Bharat Bhushan, Akhalesh Kumar Dube, Anit Kumar Jha, Ketki Rani, Akhilesh Kumar Mishra, Prateek Porwal","doi":"10.2174/0115701786267754231114064015","DOIUrl":"https://doi.org/10.2174/0115701786267754231114064015","url":null,"abstract":": Computational modeling has become a crucial tool in drug design, offering efficiency and cost-effectiveness. This paper discusses the various computational modeling techniques used in drug design and their role in enabling efficient drug discovery strategies. Molecular docking predicts the binding affinity of a small molecule to a target protein, allowing the researchers to identify potential lead compounds and optimize their interactions. Molecular dynamics simulations provide insights into protein-ligand complexes, enabling the exploration of conformational changes, binding free energies, and fundamental protein-ligand interactions. Integrating computational modeling with machine learning algorithms, such as QSAR modeling and virtual screening, enables the prediction of compound properties and prioritizes potential drug candidates. High-performance computing resources and advanced algorithms are essential for accelerating drug design workflows, with parallel computing, cloud computing, and GPU acceleration reducing computational time. The paper also addresses the challenges and limitations of computational modeling in drug design, such as the accuracy of scoring functions, protein flexibility representation, and validation of predictive models. It emphasizes the need for experimental validation and iterative refinement of computational predictions to ensure the reliability and efficacy of designed drugs.","PeriodicalId":18116,"journal":{"name":"Letters in Organic Chemistry","volume":null,"pages":null},"PeriodicalIF":0.8,"publicationDate":"2024-02-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139664594","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}
Pub Date : 2024-02-02DOI: 10.2174/0115701786286587240130114029
A. M. Rayate, M. R. Gaware
: In this paper, we have reported solvent solvent-free method for Knoevenagel condensation reaction of various aldehydes with active methylene compounds using thiourea and ammonium chloride. The developed method demonstrated high efficiency in the formation of C-C bond. The reaction proceeds smoothly under mild and solvent-free conditions and the products obtained are in excellent yield in very short duration. This method is applicable to a wide range of aldehydes with active methylene compounds.
{"title":"Thiourea-Ammonium Chloride Mediated Knoevenagel Condensation as an Intermediate in the Synthesis of Pyrimidine Scaffolds under Solvent-free Condition","authors":"A. M. Rayate, M. R. Gaware","doi":"10.2174/0115701786286587240130114029","DOIUrl":"https://doi.org/10.2174/0115701786286587240130114029","url":null,"abstract":": In this paper, we have reported solvent solvent-free method for Knoevenagel condensation reaction of various aldehydes with active methylene compounds using thiourea and ammonium chloride. The developed method demonstrated high efficiency in the formation of C-C bond. The reaction proceeds smoothly under mild and solvent-free conditions and the products obtained are in excellent yield in very short duration. This method is applicable to a wide range of aldehydes with active methylene compounds.","PeriodicalId":18116,"journal":{"name":"Letters in Organic Chemistry","volume":null,"pages":null},"PeriodicalIF":0.8,"publicationDate":"2024-02-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139664992","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}
Pub Date : 2024-02-01DOI: 10.2174/0115701786294340240129071221
Imran Ahmad, Debolina Basu
: In the current work, the Electro-Fenton (EF) based Reactive Orange 16 (RO16) dye treatment was studied and compared with central composite (CC) and Taguchi design (TD) statistical optimization tools. Color removal (RC) and COD decay (RCOD) were chosen responses for the effect of pH (A), electrolysis time (B), initial dye concentration (C), and current density (D). The facecentred CC design and L16 orthogonal array were used in the experimental procedures. At optimal conditions, the coefficient of determination (R2) values of 0.99 for CC and 0.97 for TD suggest statistical significance and good model agreement. The results of the ANOVA and Prob. > F values supported the model’s successful experimental data fitting. Taguchi method was found as an appropriate methodology for parameter percentage contributions with fewer experimental runs. Moreover, the S/N ratio charts proved to be a successful CC design replacement. The current density and pH were found to be the most important factors for the EF process. A higher biodegradability (BOD5/COD) and minimum iron concentration (0.45 mg/L) in the effluent sludge demonstrated good environmental disposal suitability. In the last, the effect of various inhibitors/scavengers (SO4 −2, PO4 −3, EDTA, etc.) on the EF process performance was also carried out.
:在当前工作中，研究了基于电-芬顿（EF）的活性橙 16（RO16）染料处理，并使用中心复合（CC）和田口设计（TD）统计优化工具进行了比较。针对 pH 值（A）、电解时间（B）、初始染料浓度（C）和电流密度（D）的影响，选择了颜色去除率（RC）和 COD 降解率（RCOD）作为响应。实验过程采用了面心 CC 设计和 L16 正交阵列。在最佳条件下，CC 和 TD 的判定系数 (R2) 分别为 0.99 和 0.97，表明统计意义显著，模型一致性良好。方差分析结果和 Prob.田口方法被认为是一种合适的方法，可以用较少的实验次数来计算参数百分比。此外，信噪比图表被证明是一种成功的 CC 设计替代方法。研究发现，电流密度和 pH 值是影响 EF 过程的最重要因素。出水污泥中较高的生物降解性（BOD5/COD）和最低的铁浓度（0.45 mg/L）证明了良好的环境处置适宜性。最后，还研究了各种抑制剂/清除剂（SO4 -2、PO4 -3、乙二胺四乙酸等）对 EF 工艺性能的影响。
{"title":"Treatment of Reactive Orange 16 Dye-Bearing Wastewater by Electro-Fenton Process with Stainless-Steel Electrodes: Statistical Optimization and Operational Analysis","authors":"Imran Ahmad, Debolina Basu","doi":"10.2174/0115701786294340240129071221","DOIUrl":"https://doi.org/10.2174/0115701786294340240129071221","url":null,"abstract":": In the current work, the Electro-Fenton (EF) based Reactive Orange 16 (RO16) dye treatment was studied and compared with central composite (CC) and Taguchi design (TD) statistical optimization tools. Color removal (RC) and COD decay (RCOD) were chosen responses for the effect of pH (A), electrolysis time (B), initial dye concentration (C), and current density (D). The facecentred CC design and L16 orthogonal array were used in the experimental procedures. At optimal conditions, the coefficient of determination (R2) values of 0.99 for CC and 0.97 for TD suggest statistical significance and good model agreement. The results of the ANOVA and Prob. > F values supported the model’s successful experimental data fitting. Taguchi method was found as an appropriate methodology for parameter percentage contributions with fewer experimental runs. Moreover, the S/N ratio charts proved to be a successful CC design replacement. The current density and pH were found to be the most important factors for the EF process. A higher biodegradability (BOD5/COD) and minimum iron concentration (0.45 mg/L) in the effluent sludge demonstrated good environmental disposal suitability. In the last, the effect of various inhibitors/scavengers (SO4 −2, PO4 −3, EDTA, etc.) on the EF process performance was also carried out.","PeriodicalId":18116,"journal":{"name":"Letters in Organic Chemistry","volume":null,"pages":null},"PeriodicalIF":0.8,"publicationDate":"2024-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139664680","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}
: In this study, an efficient method for the synthesis of one type of aromatic ether was introduced, and its antitumor activity was investigated. Specifically, (diacetoxyiodo)arene was prepared from 2-methyliodobenzene and used to oxidize the 4-nitrophenol to give the aromatic ether. Our study further found that aromatic ether has a strong apoptotic effect on U937 monocytes, suggesting that it might be developed as a new drug for the treatment of acute myeloid leukemia.
{"title":"Facile Synthesis and Antitumor Activity of o-Iodoaromatic Ether","authors":"Xiaoxia Mao, Yuying Zhang, Keyang Wang, Guiqin Zhao, Dejun Zhou, Zhengguo Cui","doi":"10.2174/0115701786262911240121105544","DOIUrl":"https://doi.org/10.2174/0115701786262911240121105544","url":null,"abstract":": In this study, an efficient method for the synthesis of one type of aromatic ether was introduced, and its antitumor activity was investigated. Specifically, (diacetoxyiodo)arene was prepared from 2-methyliodobenzene and used to oxidize the 4-nitrophenol to give the aromatic ether. Our study further found that aromatic ether has a strong apoptotic effect on U937 monocytes, suggesting that it might be developed as a new drug for the treatment of acute myeloid leukemia.","PeriodicalId":18116,"journal":{"name":"Letters in Organic Chemistry","volume":null,"pages":null},"PeriodicalIF":0.8,"publicationDate":"2024-01-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139580403","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}
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