Synthetic Communications最新文献

Synthesis, characterization, crystal structure and anti-proliferative properties of curcumin mimic conjugates 姜黄素模拟物的合成、表征、晶体结构和抗增殖性能

IF 1.8 3区化学

Synthetic Communications Pub Date : 2025-06-24 DOI: 10.1080/00397911.2025.2520609

Aisha A. Alsfouk (Data curation Funding acquisition Methodology Validation Writing – original draft) , Benson M. Kariuki (Data curation Formal analysis Investigation Methodology Resources Software Validation Visualization Writing – original draft) , Asmaa Saleh (Data curation Funding acquisition Project administration Validation Visualization Writing – original draft) , Aladdin M. Srour (Conceptualization Investigation Methodology Supervision Validation Visualization Writing – original draft Writing – review & editing)

{"title":"Synthesis, characterization, crystal structure and anti-proliferative properties of curcumin mimic conjugates","authors":"Aisha A. Alsfouk (Data curation Funding acquisition Methodology Validation Writing – original draft) , Benson M. Kariuki (Data curation Formal analysis Investigation Methodology Resources Software Validation Visualization Writing – original draft) , Asmaa Saleh (Data curation Funding acquisition Project administration Validation Visualization Writing – original draft) , Aladdin M. Srour (Conceptualization Investigation Methodology Supervision Validation Visualization Writing – original draft Writing – review & editing)","doi":"10.1080/00397911.2025.2520609","DOIUrl":"10.1080/00397911.2025.2520609","url":null,"abstract":"<div><div>Three novel 4-piperidone-based derivatives (<strong>3a–c</strong>) were synthesized utilizing the base-catalyzed condensation method (KOH/EtOH) with aromatic aldehydes (<strong>2a–c</strong>) featuring secondary amine rings, specifically piperidine, morpholine, and methyl piperazine. The three newly synthesized derivatives were characterized through X-ray crystallography, and their anti-proliferative effects were assessed against three different human cancer cell lines: breast carcinoma (MCF-7), liver cancer (HepG-2), and colorectal carcinoma (HCT-116), along with a normal cell line (RPE1), following the MTT assay procedure. Among them, compound <strong>3c</strong> demonstrated the highest efficacy against all tested cell lines, demonstrating IC<sub>50</sub> = 1.07 ± 0.04 μM for MCF-7 and 2.55 ± 0.07 μM for HepG-2, compared to the standard reference, Doxorubicin, which had IC<sub>50</sub> = 5.38 ± 0.05 μM and 4.25 ± 0.01 μM, respectively. Moreover, a molecular docking study confirmed the stable interaction of compound <strong>3c</strong> within the ATP binding site of human cyclin-dependent kinase 2 (CDK2). This study introduces three promising intermediates for further research in medicinal chemistry.</div></div>","PeriodicalId":22119,"journal":{"name":"Synthetic Communications","volume":"55 13","pages":"Pages 1029-1043"},"PeriodicalIF":1.8,"publicationDate":"2025-06-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144510863","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"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

A one-pot route to novel 3-{1-([5-amino-7-(arylamino)-6-cyano-7H-[1,4]oxaphosphinino[2,3-d]thiazol-2-yl]hydrazinyl)ethylidene}-2H-chromen-2-one: Synthesis, cytotoxic activities, apoptosis, and cell cycle studies 新型3-{1-（[5-氨基-7-（芳基氨基）-6-氰基- 7h -[1,4]草磷酰[2,3-d]噻唑-2-基]肼基）乙基}- 2h - chromen2 -one：合成、细胞毒性活性、细胞凋亡和细胞周期研究

IF 1.8 3区化学

Synthetic Communications Pub Date : 2025-06-24 DOI: 10.1080/00397911.2025.2521830

Wafa A. Bawazir (Investigation Methodology) , Tarik E. Ali (Conceptualization Funding acquisition Supervision Writing – original draft Writing – review & editing) , Mohammed A. Assiri (Formal analysis Software) , Serag E. I. Elbehairi (Methodology Validation) , Mohamed Abdel-Megid (Visualization Writing – review & editing)

{"title":"A one-pot route to novel 3-{1-([5-amino-7-(arylamino)-6-cyano-7H-[1,4]oxaphosphinino[2,3-d]thiazol-2-yl]hydrazinyl)ethylidene}-2H-chromen-2-one: Synthesis, cytotoxic activities, apoptosis, and cell cycle studies","authors":"Wafa A. Bawazir (Investigation Methodology) , Tarik E. Ali (Conceptualization Funding acquisition Supervision Writing – original draft Writing – review & editing) , Mohammed A. Assiri (Formal analysis Software) , Serag E. I. Elbehairi (Methodology Validation) , Mohamed Abdel-Megid (Visualization Writing – review & editing)","doi":"10.1080/00397911.2025.2521830","DOIUrl":"10.1080/00397911.2025.2521830","url":null,"abstract":"<div><div>An innovative and efficient one-pot approach has been established for the synthesis of 3-{1-([5-amino-7-(arylamino)-6-cyano-7<em>H</em>-[1,4]oxaphosphinino[2,3-d]thiazol-2-yl]hydrazinyl)ethylidene}-2<em>H</em>-chromen-2-one (<strong>2a–h</strong>) using aromatic amine, phosphorus trichloride, malononitrile, and 3-{[1-(4-oxo-5<em>H</em>-thiazol-2-yl)hydrazinyl]ethylidene}-2<em>H</em>-chromen-2-one with triethylamine. This method is efficient and straightforward, offering high yields, easy product isolation, and minimal waste. The cytotoxic properties against PC3, LS174T, and HepG2 cancer cell lines revealed promising activity for compounds <strong>2d</strong> and <strong>2e</strong> (fluorine and chlorine substitutions), comparable to Tivozanib. Flow cytometry indicated that these bioactive compounds significantly increased late apoptosis and halted cell cycle progression at S and G2 phases, demonstrating their potential as anticancer agents. Both compounds <strong>2d</strong> and <strong>2e</strong> were then subjected to a molecular docking experiment to see how they bind with VEGFR-2 receptor.</div></div>","PeriodicalId":22119,"journal":{"name":"Synthetic Communications","volume":"55 13","pages":"Pages 1007-1028"},"PeriodicalIF":1.8,"publicationDate":"2025-06-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144510864","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"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

A sustainable approach for one-pot, multicomponent synthesis of 2-amino-4H-chromenes using bleach 漂白剂一锅多组分合成2-氨基- 4h -铬的可持续方法

IF 1.8 3区化学

Synthetic Communications Pub Date : 2025-06-21 DOI: 10.1080/00397911.2025.2521701

Nikita Shinde (Methodology Project administration Writing – original draft) , Lina Jadhav (Investigation Validation) , Mayuri B. Thorat (Writing – review & editing), Krantisagar More (Resources Supervision) , Yatin U. Gadkari (Conceptualization Methodology Project administration Writing – review & editing)

引用次数: 0

One-pot synthesis of amides from aryloyl peroxides and aldimines in dimethyl sulfoxide 二甲基亚砜中一锅法合成芳酰过氧化物和醛胺酰胺

IF 1.8 3区化学

Synthetic Communications Pub Date : 2025-06-18 DOI: 10.1080/00397911.2025.2508211

Xinyun Zhao (Funding acquisition Writing – review & editing) , Dongli Li (Data curation) , Tsunghsueh Wu (Formal analysis) , Xiaoqiang Hu (Methodology) , Xi Chen (Formal analysis) , Lamei Wu (Formal analysis) , Zhan Zhang (Formal analysis)

{"title":"One-pot synthesis of amides from aryloyl peroxides and aldimines in dimethyl sulfoxide","authors":"Xinyun Zhao (Funding acquisition Writing – review & editing) , Dongli Li (Data curation) , Tsunghsueh Wu (Formal analysis) , Xiaoqiang Hu (Methodology) , Xi Chen (Formal analysis) , Lamei Wu (Formal analysis) , Zhan Zhang (Formal analysis)","doi":"10.1080/00397911.2025.2508211","DOIUrl":"10.1080/00397911.2025.2508211","url":null,"abstract":"<div><div>A novel method for amide synthesis from aldimines using an aryloyl peroxide/DMSO system has been developed. The acyl groups of the resulting amides are derived from the aryloyl peroxide, while the <em>N</em>-containing motifs originate from the aldimines. Mechanistic investigations reveal that the aryloyl peroxide reacts with DMSO to form an anhydride, which is partially hydrolyzed to produce a carboxylic acid. This acid catalyzes the hydrolysis of aldimines to controllably release amines, which then react with the anhydride to selectively form amides. This approach offers controlled reaction and product selectivity, avoiding byproduct formation from direct arylamine oxidation by BPO. This mild one-pot method not only provides a route for the synthesis of amides from aldimines, but also demonstrates the feasibility of synthesizing amides from amines, thereby expanding the scope of organic synthesis strategies.</div></div>","PeriodicalId":22119,"journal":{"name":"Synthetic Communications","volume":"55 12","pages":"Pages 901-915"},"PeriodicalIF":1.8,"publicationDate":"2025-06-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144510959","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"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

Convenient synthesis of novel C2-symmetric bisoxazolidine derivatives containing a sulfonamide moiety 含磺酰胺部分的新型c2对称双恶唑烷衍生物的便捷合成

IF 1.8 3区化学

Synthetic Communications Pub Date : 2025-06-18 DOI: 10.1080/00397911.2025.2505905

L. Boughani (Conceptualization Investigation Methodology Validation Visualization Writing – original draft Writing – review & editing) , D. Bouchouk (Methodology Visualization) , T. Abbaz (Methodology Visualization) , A. Bendjeddou (Methodology Visualization) , Z. Regainia (Conceptualization Methodology Supervision)

引用次数: 0

Design, synthesis, and in silico studies of pyrazolyl-thiazole and thiazolidinone hybrids as potential antiproliferative agents 吡唑基噻唑和噻唑烷酮杂合体作为潜在抗增殖剂的设计、合成和硅研究

IF 1.8 3区化学

Synthetic Communications Pub Date : 2025-06-18 DOI: 10.1080/00397911.2025.2511819

Sayed K. Ramadan (Conceptualization Data curation Investigation Methodology Validation Visualization Writing – original draft Writing – review & editing) , Amira T. Ali (Investigation Methodology Writing – original draft Writing – review & editing) , Sobhi M. Gomha (Data curation Investigation Supervision Writing – review & editing) , Eman A. E. El-Helw (Conceptualization Investigation Methodology Writing – original draft Writing – review & editing)

{"title":"Design, synthesis, and in silico studies of pyrazolyl-thiazole and thiazolidinone hybrids as potential antiproliferative agents","authors":"Sayed K. Ramadan (Conceptualization Data curation Investigation Methodology Validation Visualization Writing – original draft Writing – review & editing) , Amira T. Ali (Investigation Methodology Writing – original draft Writing – review & editing) , Sobhi M. Gomha (Data curation Investigation Supervision Writing – review & editing) , Eman A. E. El-Helw (Conceptualization Investigation Methodology Writing – original draft Writing – review & editing)","doi":"10.1080/00397911.2025.2511819","DOIUrl":"10.1080/00397911.2025.2511819","url":null,"abstract":"<div><div>Breast and liver cancers are the most common causes of cancer death and finding new anticancer agents is critical. Inspired by their antitumor potential, thiazole and thiazolidinone derivatives bearing a pyrazole core were prepared from thiosemicarbazone unit through reactions with carbon electrophiles. Compared to doxorubicin and roscovitine, <em>in vitro</em>, antiproliferative activity against MCF7 and HepG2 cancer cell panels implied the most potency of 2,4-dihydroxybenzylidene- and 4-dimethylaminobenzylidene-thiazolidinone, being capable of powerful interactions with protein receptors. In density functional theory simulation, the dimethylaminobenzylidine-thiazolidine exhibited the lowest energy gap and highest softness values. Consistently, the superlative docking score toward CDK2 protein (PDB ID: 2A4L) was shown by later compound through hydrogen bonding, arene-hydrogen, and arene-cation interactions with key nucleobases and amino acids of CDK2 protein which might be potential CDK2 inhibitor. According to ADME study, these compounds showed good lipophilicity and oral bioavailability. This work may contribute to the advancing of new potent antiproliferative agents.</div></div>","PeriodicalId":22119,"journal":{"name":"Synthetic Communications","volume":"55 12","pages":"Pages 931-951"},"PeriodicalIF":1.8,"publicationDate":"2025-06-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144510960","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"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

Face index computation of certain polycyclic aromatic hydrocarbons 某些多环芳烃面指数的计算

IF 1.8 3区化学

Synthetic Communications Pub Date : 2025-06-18 DOI: 10.1080/00397911.2025.2509114

Shriya Negi (Conceptualization Investigation Validation Writing – original draft Writing – review & editing) , Jai Parkash (Investigation Methodology Writing – review & editing) , Vijay Kumar Bhat (Conceptualization Investigation Supervision Writing – original draft Writing – review & editing)

{"title":"Face index computation of certain polycyclic aromatic hydrocarbons","authors":"Shriya Negi (Conceptualization Investigation Validation Writing – original draft Writing – review & editing) , Jai Parkash (Investigation Methodology Writing – review & editing) , Vijay Kumar Bhat (Conceptualization Investigation Supervision Writing – original draft Writing – review & editing)","doi":"10.1080/00397911.2025.2509114","DOIUrl":"10.1080/00397911.2025.2509114","url":null,"abstract":"<div><div>The face index is a topological descriptor that provides insights into the molecular architecture of PAHs, which are significant due to their environmental persistence and potential health impacts. By analyzing the graphical representations of these compounds, we derive mathematical expressions for their face indices, highlighting the relationships between their structural features and chemical properties. Our findings contribute to a deeper understanding of how molecular structure influences the behavior of PAHs, paving the way for further research in both theoretical and applied chemistry contexts. This study not only enhances the characterization of complex PAH structures but also serves as a foundation for future investigations into their environmental and toxicological implications. We focus on Hexa-cata-hexa-benzocoronene and Dodeca-benzo-circumcoronene and derive analytical expressions for their face index based on their molecular graphs.</div></div>","PeriodicalId":22119,"journal":{"name":"Synthetic Communications","volume":"55 12","pages":"Pages 916-930"},"PeriodicalIF":1.8,"publicationDate":"2025-06-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144510958","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"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

Recent advancements of pyrimidine chemistry thriving deeper into drug discovery 最近的进展嘧啶化学蓬勃发展，深入到药物发现

IF 1.8 3区化学

Synthetic Communications Pub Date : 2025-06-18 DOI: 10.1080/00397911.2025.2487080

Glanish Jude Martis (Software Writing – original draft) , Sneha O (Writing – original draft) , Rajkumar Bhat D (Writing – review & editing) , Praveen S. Mugali (Writing – review & editing)

引用次数: 0

Pyrazole-Sulfone hybridization via silver-catalyzed regioselective aza-Michael addition of pyrazoles to vinyl sulfones: Synthesis of N-sulfonylethylated pyrazoles 银催化吡唑与乙烯基砜的区域选择性杂化：n -磺基乙基化吡唑的合成

IF 1.8 3区化学

Synthetic Communications Pub Date : 2025-06-12 DOI: 10.1080/00397911.2025.2518387

Xue Zhang (Conceptualization Writing – original draft Writing – review & editing) , Yang Song (Data curation Formal analysis) , Yutong Peng (Investigation) , Dakang Zhu (Methodology) , Wanxin Zhang (Investigation) , Haifeng Yu (Conceptualization) , Xiaobo Zhao (Project administration)

引用次数: 0

A novel strategy for the efficient synthesis of Erianin 一种高效合成羊角苷的新方法

IF 1.8 3区化学

Synthetic Communications Pub Date : 2025-05-16 DOI: 10.1080/00397911.2025.2505903

Wenpei Zhang (Data curation Investigation Methodology Writing – original draft Writing – review & editing) , Xinyue Pan (Investigation) , Jie He (Supervision) , Yirong Lin (Visualization) , Fengyang Zhang (Validation) , Li Guo (Validation) , Jieqing Liu (Conceptualization Funding acquisition Project administration Resources)

引用次数: 0