Pub Date : 2023-12-12DOI: 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
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...
{"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}
Pub Date : 2023-12-11DOI: 10.1080/14756366.2023.2286435
Lijie Sima, Zhongyuan Wang, Ling Yu, Youli Hou, Dongsheng Zhao, Bilan Luo, Weike Liao, Xinfu Liu
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...
{"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}
Pub Date : 2023-12-11DOI: 10.1080/14756366.2023.2290911
Rajath Cyriac, Kwangho Lee
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...
{"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}
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...
{"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}
Pub Date : 2023-12-11DOI: 10.1080/14756366.2023.2284113
Mateusz Olszewski, Maryna Stasevych, Viktor Zvarych, Natalia Maciejewska
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...
{"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}
Pub Date : 2023-12-11DOI: 10.1080/14756366.2023.2288548
Mohammad Altamimi, Saeed Ali Syed, Burak Tuzun, Mohammad Rashid Alhazani, Osamah Alnemer, Ahmed Bari
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...
{"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}
Pub Date : 2023-12-11DOI: 10.1080/14756366.2023.2291336
Dimitrios Tsikas
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 ...
{"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}
Pub Date : 2023-12-11DOI: 10.1080/14756366.2023.2290912
Yajun Liu, Chenyao Li, Yajing Li, Shuming Zhang, Ning Zhang, Xiaobo Bian, Shutao Tan
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...
{"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}
Pub Date : 2023-12-07DOI: 10.1080/14756366.2023.2286925
Yusuf Akbaba, Fatma Necmiye Kacı, Mehmet Enes Arslan, Süleyman Göksü, Adil Mardinoğlu, Hasan Türkez
Cancer and antibiotic-resistant bacterial infections are significant global health challenges. The resistance developed in cancer treatments intensifies therapeutic difficulties. In addressing thes...
{"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}
Pub Date : 2023-12-07DOI: 10.1080/14756366.2023.2287990
Pengming Pan, Dengbo Ji, Zhongjun Li, Xiangbao Meng
Doublecortin-like kinase 1 (DCLK) is a microtubule-associated serine/threonine kinase that is upregulated in a wide range of cancers and is believed to be related to tumour growth and development. ...
{"title":"Design and synthesis of doublecortin-like kinase 1 inhibitors and their bioactivity evaluation","authors":"Pengming Pan, Dengbo Ji, Zhongjun Li, Xiangbao Meng","doi":"10.1080/14756366.2023.2287990","DOIUrl":"https://doi.org/10.1080/14756366.2023.2287990","url":null,"abstract":"Doublecortin-like kinase 1 (DCLK) is a microtubule-associated serine/threonine kinase that is upregulated in a wide range of cancers and is believed to be related to tumour growth and development. ...","PeriodicalId":15769,"journal":{"name":"Journal of Enzyme Inhibition and Medicinal Chemistry","volume":"40 1","pages":""},"PeriodicalIF":5.6,"publicationDate":"2023-12-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138552783","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}
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