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Journal of Enzyme Inhibition and Medicinal Chemistry最新文献

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Development of iminosugar-based glycosidase inhibitors as drug candidates for SARS-CoV-2 virus via molecular modelling and in vitro studies 通过分子建模和体外研究开发亚氨基糖基糖苷酶抑制剂，作为 SARS-CoV-2 病毒的候选药物
IF 5.6 2区 医学
Journal of Enzyme Inhibition and Medicinal Chemistry Pub Date : 2023-12-12 DOI: 10.1080/14756366.2023.2289007
Zorana Ferjancic, Filip Bihelovic, Bojan Vulovic, Radomir Matovic, Milena Trmcic, Aleksandar Jankovic, Milos Pavlovic, Filip Djurkovic, Radivoje Prodanovic, Aleksandra Djurdjevic Djelmas, Nevena Kalicanin, Mario Zlatovic, Dusan Sladic, Thomas Vallet, Marco Vignuzzi, Radomir N. Saicic
{"title":"Development of iminosugar-based glycosidase inhibitors as drug candidates for SARS-CoV-2 virus via molecular modelling and in vitro studies","authors":"Zorana Ferjancic, Filip Bihelovic, Bojan Vulovic, Radomir Matovic, Milena Trmcic, Aleksandar Jankovic, Milos Pavlovic, Filip Djurkovic, Radivoje Prodanovic, Aleksandra Djurdjevic Djelmas, Nevena Kalicanin, Mario Zlatovic, Dusan Sladic, Thomas Vallet, Marco Vignuzzi, Radomir N. Saicic","doi":"10.1080/14756366.2023.2289007","DOIUrl":"https://doi.org/10.1080/14756366.2023.2289007","url":null,"abstract":"We developed new iminosugar-based glycosidase inhibitors against SARS-CoV-2. Known drugs (miglustat, migalastat, miglitol, and swainsonine) were chosen as lead compounds to develop three classes of...","PeriodicalId":15769,"journal":{"name":"Journal of Enzyme Inhibition and Medicinal Chemistry","volume":"36 1","pages":""},"PeriodicalIF":5.6,"publicationDate":"2023-12-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138689073","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Novel isobavachalcone derivatives induce apoptosis and necroptosis in human non-small cell lung cancer H1975 cells 新型异巴夏尔酮衍生物诱导人非小细胞肺癌 H1975 细胞凋亡和坏死
IF 5.6 2区 医学
Journal of Enzyme Inhibition and Medicinal Chemistry Pub Date : 2023-12-12 DOI: 10.1080/14756366.2023.2292006
Jie Chen, Long Zhao, Meng-Fan Xu, Di Huang, Xiao-Long Sun, Yu-Xin Zhang, Hong-Mei Li, Cheng-Zhu Wu
{"title":"Novel isobavachalcone derivatives induce apoptosis and necroptosis in human non-small cell lung cancer H1975 cells","authors":"Jie Chen, Long Zhao, Meng-Fan Xu, Di Huang, Xiao-Long Sun, Yu-Xin Zhang, Hong-Mei Li, Cheng-Zhu Wu","doi":"10.1080/14756366.2023.2292006","DOIUrl":"https://doi.org/10.1080/14756366.2023.2292006","url":null,"abstract":"In this study, seventeen isobavachalcone (IBC) derivatives (1–17) were synthesised, and evaluated for their cytotoxic activity against three human lung cancer cell lines. Among these derivatives, c...","PeriodicalId":15769,"journal":{"name":"Journal of Enzyme Inhibition and Medicinal Chemistry","volume":"86 1","pages":""},"PeriodicalIF":5.6,"publicationDate":"2023-12-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138688926","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Discovery of LAH-1 as potent c-Met inhibitor for the treatment of non-small cell lung cancer 发现用于治疗非小细胞肺癌的强效 c-Met 抑制剂 LAH-1
IF 5.6 2区 医学
Journal of Enzyme Inhibition and Medicinal Chemistry Pub Date : 2023-12-11 DOI: 10.1080/14756366.2023.2286435
Lijie Sima, Zhongyuan Wang, Ling Yu, Youli Hou, Dongsheng Zhao, Bilan Luo, Weike Liao, Xinfu Liu
{"title":"Discovery of LAH-1 as potent c-Met inhibitor for the treatment of non-small cell lung cancer","authors":"Lijie Sima, Zhongyuan Wang, Ling Yu, Youli Hou, Dongsheng Zhao, Bilan Luo, Weike Liao, Xinfu Liu","doi":"10.1080/14756366.2023.2286435","DOIUrl":"https://doi.org/10.1080/14756366.2023.2286435","url":null,"abstract":"Dysregulated HGF/c-Met pathway has been implicated in multiple human cancers and has become an attractive target for cancer intervention. Herein, we report the discovery of N-(3-fluoro-4-((2-(3-hyd...","PeriodicalId":15769,"journal":{"name":"Journal of Enzyme Inhibition and Medicinal Chemistry","volume":"16 1","pages":""},"PeriodicalIF":5.6,"publicationDate":"2023-12-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138566604","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Glutaminase inhibition as potential cancer therapeutics: current status and future applications 作为潜在癌症疗法的谷氨酰胺酶抑制剂：现状与未来应用
IF 5.6 2区 医学
Journal of Enzyme Inhibition and Medicinal Chemistry Pub Date : 2023-12-11 DOI: 10.1080/14756366.2023.2290911
Rajath Cyriac, Kwangho Lee
{"title":"Glutaminase inhibition as potential cancer therapeutics: current status and future applications","authors":"Rajath Cyriac, Kwangho Lee","doi":"10.1080/14756366.2023.2290911","DOIUrl":"https://doi.org/10.1080/14756366.2023.2290911","url":null,"abstract":"Alterations in normal metabolic processes are defining features of cancer. Glutamine, an abundant amino acid in the human blood, plays a critical role in regulating several biosynthetic and bioener...","PeriodicalId":15769,"journal":{"name":"Journal of Enzyme Inhibition and Medicinal Chemistry","volume":"17 1","pages":""},"PeriodicalIF":5.6,"publicationDate":"2023-12-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138689078","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Design, synthesis, and biological evaluation of piperazine derivatives involved in the 5-HT1AR/BDNF/PKA pathway 参与 5-HT1AR/BDNF/PKA 通路的哌嗪衍生物的设计、合成和生物学评价
IF 5.6 2区 医学
Journal of Enzyme Inhibition and Medicinal Chemistry Pub Date : 2023-12-11 DOI: 10.1080/14756366.2023.2286183
Hao Zhou, Mengjiao Li, Hui Liu, Zheng Liu, Xuekun Wang, Shiben Wang
{"title":"Design, synthesis, and biological evaluation of piperazine derivatives involved in the 5-HT1AR/BDNF/PKA pathway","authors":"Hao Zhou, Mengjiao Li, Hui Liu, Zheng Liu, Xuekun Wang, Shiben Wang","doi":"10.1080/14756366.2023.2286183","DOIUrl":"https://doi.org/10.1080/14756366.2023.2286183","url":null,"abstract":"In this study, four series of piperazine derivatives were designed, synthesised and subjected to biological test, and compound 6a with potential antidepressant activity was obtained. An affinity as...","PeriodicalId":15769,"journal":{"name":"Journal of Enzyme Inhibition and Medicinal Chemistry","volume":"15 1","pages":""},"PeriodicalIF":5.6,"publicationDate":"2023-12-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138629454","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
9,10-Dioxoanthracenyldithiocarbamates effectively inhibit the proliferation of non-small cell lung cancer by targeting multiple protein tyrosine kinases 9,10-二氧代蒽二硫代氨基甲酸酯通过靶向多种蛋白酪氨酸激酶有效抑制非小细胞肺癌的增殖
IF 5.6 2区 医学
Journal of Enzyme Inhibition and Medicinal Chemistry Pub Date : 2023-12-11 DOI: 10.1080/14756366.2023.2284113
Mateusz Olszewski, Maryna Stasevych, Viktor Zvarych, Natalia Maciejewska
{"title":"9,10-Dioxoanthracenyldithiocarbamates effectively inhibit the proliferation of non-small cell lung cancer by targeting multiple protein tyrosine kinases","authors":"Mateusz Olszewski, Maryna Stasevych, Viktor Zvarych, Natalia Maciejewska","doi":"10.1080/14756366.2023.2284113","DOIUrl":"https://doi.org/10.1080/14756366.2023.2284113","url":null,"abstract":"Anthraquinones have attracted considerable interest in the realm of cancer treatment owing to their potent anticancer properties. This study evaluates the potential of a series of new anthraquinone...","PeriodicalId":15769,"journal":{"name":"Journal of Enzyme Inhibition and Medicinal Chemistry","volume":"16 1","pages":""},"PeriodicalIF":5.6,"publicationDate":"2023-12-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138566835","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Synthesis biological evaluation and molecular docking of isatin hybrids as anti-cancer and anti-microbial agents 作为抗癌剂和抗微生物剂的靛红混合物的合成、生物学评价和分子对接
IF 5.6 2区 医学
Journal of Enzyme Inhibition and Medicinal Chemistry Pub Date : 2023-12-11 DOI: 10.1080/14756366.2023.2288548
Mohammad Altamimi, Saeed Ali Syed, Burak Tuzun, Mohammad Rashid Alhazani, Osamah Alnemer, Ahmed Bari
{"title":"Synthesis biological evaluation and molecular docking of isatin hybrids as anti-cancer and anti-microbial agents","authors":"Mohammad Altamimi, Saeed Ali Syed, Burak Tuzun, Mohammad Rashid Alhazani, Osamah Alnemer, Ahmed Bari","doi":"10.1080/14756366.2023.2288548","DOIUrl":"https://doi.org/10.1080/14756366.2023.2288548","url":null,"abstract":"Isatin, known as 1H-indole-2,3-dione, was originally recognised as a synthetic molecule until its discovery in the fruits of the cannonball tree, Couroupita guianensis. It is naturally occurring in...","PeriodicalId":15769,"journal":{"name":"Journal of Enzyme Inhibition and Medicinal Chemistry","volume":"3 1","pages":""},"PeriodicalIF":5.6,"publicationDate":"2023-12-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138566511","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Acetazolamide and human carbonic anhydrases: retrospect, review and discussion of an intimate relationship 乙酰唑胺和人体碳酸酐酶：亲密关系的回顾、评述和讨论
IF 5.6 2区 医学
Journal of Enzyme Inhibition and Medicinal Chemistry Pub Date : 2023-12-11 DOI: 10.1080/14756366.2023.2291336
Dimitrios Tsikas
{"title":"Acetazolamide and human carbonic anhydrases: retrospect, review and discussion of an intimate relationship","authors":"Dimitrios Tsikas","doi":"10.1080/14756366.2023.2291336","DOIUrl":"https://doi.org/10.1080/14756366.2023.2291336","url":null,"abstract":"Acetazolamide (AZM) is a strong pharmacological sulphonamide-type (R-SO2-NH2, pKa 7.2) inhibitor of the activity of several carbonic anhydrase (CA) isoforms, notably of renal CA II (Ki, 12 nM) and ...","PeriodicalId":15769,"journal":{"name":"Journal of Enzyme Inhibition and Medicinal Chemistry","volume":"2 1","pages":""},"PeriodicalIF":5.6,"publicationDate":"2023-12-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138566615","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Ligand-based pharmacophore modelling, structure optimisation, and biological evaluation for the identification of 2-heteroarylthio-N-arylacetamides as novel HSP90 C-terminal inhibitors 基于配体的药效学建模、结构优化和生物学评价，鉴定作为新型 HSP90 C 端抑制剂的 2-heteroarylthio-N-arylacetamides
IF 5.6 2区 医学
Journal of Enzyme Inhibition and Medicinal Chemistry Pub Date : 2023-12-11 DOI: 10.1080/14756366.2023.2290912
Yajun Liu, Chenyao Li, Yajing Li, Shuming Zhang, Ning Zhang, Xiaobo Bian, Shutao Tan
{"title":"Ligand-based pharmacophore modelling, structure optimisation, and biological evaluation for the identification of 2-heteroarylthio-N-arylacetamides as novel HSP90 C-terminal inhibitors","authors":"Yajun Liu, Chenyao Li, Yajing Li, Shuming Zhang, Ning Zhang, Xiaobo Bian, Shutao Tan","doi":"10.1080/14756366.2023.2290912","DOIUrl":"https://doi.org/10.1080/14756366.2023.2290912","url":null,"abstract":"Targeting Heat shock protein 90 (HSP90) C-terminus is an important strategy to develop HSP90 inhibitors without inducing heat shock response. The development of C-terminal inhibitors, however, is h...","PeriodicalId":15769,"journal":{"name":"Journal of Enzyme Inhibition and Medicinal Chemistry","volume":"88 1","pages":""},"PeriodicalIF":5.6,"publicationDate":"2023-12-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138630227","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Novel tetrahydronaphthalen-1-yl-phenethyl ureas: synthesis and dual antibacterial-anticancer activities 新型四氢萘-1-基-苯乙基脲：合成与双重抗菌抗癌活性
IF 5.6 2区 医学
Journal of Enzyme Inhibition and Medicinal Chemistry Pub Date : 2023-12-07 DOI: 10.1080/14756366.2023.2286925
Yusuf Akbaba, Fatma Necmiye Kacı, Mehmet Enes Arslan, Süleyman Göksü, Adil Mardinoğlu, Hasan Türkez
{"title":"Novel tetrahydronaphthalen-1-yl-phenethyl ureas: synthesis and dual antibacterial-anticancer activities","authors":"Yusuf Akbaba, Fatma Necmiye Kacı, Mehmet Enes Arslan, Süleyman Göksü, Adil Mardinoğlu, Hasan Türkez","doi":"10.1080/14756366.2023.2286925","DOIUrl":"https://doi.org/10.1080/14756366.2023.2286925","url":null,"abstract":"Cancer and antibiotic-resistant bacterial infections are significant global health challenges. The resistance developed in cancer treatments intensifies therapeutic difficulties. In addressing thes...","PeriodicalId":15769,"journal":{"name":"Journal of Enzyme Inhibition and Medicinal Chemistry","volume":"17 1","pages":""},"PeriodicalIF":5.6,"publicationDate":"2023-12-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138562302","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
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