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| Format: | Artículo científico |
| Sprache: | en |
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Bioorganic chemistry
2025
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| Online-Zugang: | https://pubmed.ncbi.nlm.nih.gov/40383016/ |
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| author | Chen, Xiaohui Li, Rongna Qiu, Yingkun Lin, Fanhong Chen, Shutong Li, Xiaodan Sun, Hui Jiang, Guanmin Fang, Hua Qin, Jingbo Fang, Meijuan |
| author_facet | Chen, Xiaohui Li, Rongna Qiu, Yingkun Lin, Fanhong Chen, Shutong Li, Xiaodan Sun, Hui Jiang, Guanmin Fang, Hua Qin, Jingbo Fang, Meijuan Chen, Xiaohui Li, Rongna Qiu, Yingkun Lin, Fanhong Chen, Shutong Li, Xiaodan Sun, Hui Jiang, Guanmin Fang, Hua Qin, Jingbo Fang, Meijuan |
| collection | PubMed - marine biology |
| contents | Design, synthesis, and biological evaluation of N-(2-amino-phenyl)-5-(4-aryl- pyrimidin-2-yl) amino)-1H-indole-2-carboxamide derivatives as novel inhibitors of CDK9 and class I HDACs for cancer treatment. Chen, Xiaohui Li, Rongna Qiu, Yingkun Lin, Fanhong Chen, Shutong Li, Xiaodan Sun, Hui Jiang, Guanmin Fang, Hua Qin, Jingbo Fang, Meijuan Humans Cyclin-Dependent Kinase 9 Histone Deacetylase Inhibitors Antineoplastic Agents Structure-Activity Relationship Drug Design Drug Screening Assays, Antitumor Cell Proliferation Molecular Structure Histone Deacetylases Indoles Dose-Response Relationship, Drug Animals Protein Kinase Inhibitors Mice Apoptosis Cell Line, Tumor Molecular Docking Simulation The mechanisms underlying transcriptional dysregulation in tumorigenesis have received considerable attention as promising therapeutic targets to combat human cancer. Cyclin-dependent kinase 9 (CDK9) and class I histone deacetylases (HDACs) are significant therapeutic targets due to their pivotal roles in the dysregulated transcriptional programs characteristic of many cancers. Furthermore, the combinatorial transcriptional therapy with CDK9 and class I HDAC inhibitors has been shown to have a synergistic anticancer effect. In this study, a series of novel N-(2-amino-phenyl)-5-(4-aryl-pyrimidin-2-yl) amino)-1H-indole-2-carboxamide derivatives were designed and synthesized as novel dual-functional inhibitors targeting CDK9 and HDAC signaling pathways for cancer treatment. Among the synthesized compounds, 13ea demonstrated potent anti-proliferative activities (IC |
| format | Artículo científico |
| id | pubmed_40383016 |
| institution | PubMed |
| language | en |
| publishDate | 2025 |
| publisher | Bioorganic chemistry |
| record_format | pubmed |
| spellingShingle | Design, synthesis, and biological evaluation of N-(2-amino-phenyl)-5-(4-aryl- pyrimidin-2-yl) amino)-1H-indole-2-carboxamide derivatives as novel inhibitors of CDK9 and class I HDACs for cancer treatment. Chen, Xiaohui Li, Rongna Qiu, Yingkun Lin, Fanhong Chen, Shutong Li, Xiaodan Sun, Hui Jiang, Guanmin Fang, Hua Qin, Jingbo Fang, Meijuan Humans Cyclin-Dependent Kinase 9 Histone Deacetylase Inhibitors Antineoplastic Agents Structure-Activity Relationship Drug Design Drug Screening Assays, Antitumor Cell Proliferation Molecular Structure Histone Deacetylases Indoles Dose-Response Relationship, Drug Animals Protein Kinase Inhibitors Mice Apoptosis Cell Line, Tumor Molecular Docking Simulation Design, synthesis, and biological evaluation of N-(2-amino-phenyl)-5-(4-aryl- pyrimidin-2-yl) amino)-1H-indole-2-carboxamide derivatives as novel inhibitors of CDK9 and class I HDACs for cancer treatment. Chen, Xiaohui Li, Rongna Qiu, Yingkun Lin, Fanhong Chen, Shutong Li, Xiaodan Sun, Hui Jiang, Guanmin Fang, Hua Qin, Jingbo Fang, Meijuan Humans Cyclin-Dependent Kinase 9 Histone Deacetylase Inhibitors Antineoplastic Agents Structure-Activity Relationship Drug Design Drug Screening Assays, Antitumor Cell Proliferation Molecular Structure Histone Deacetylases Indoles Dose-Response Relationship, Drug Animals Protein Kinase Inhibitors Mice Apoptosis Cell Line, Tumor Molecular Docking Simulation The mechanisms underlying transcriptional dysregulation in tumorigenesis have received considerable attention as promising therapeutic targets to combat human cancer. Cyclin-dependent kinase 9 (CDK9) and class I histone deacetylases (HDACs) are significant therapeutic targets due to their pivotal roles in the dysregulated transcriptional programs characteristic of many cancers. Furthermore, the combinatorial transcriptional therapy with CDK9 and class I HDAC inhibitors has been shown to have a synergistic anticancer effect. In this study, a series of novel N-(2-amino-phenyl)-5-(4-aryl-pyrimidin-2-yl) amino)-1H-indole-2-carboxamide derivatives were designed and synthesized as novel dual-functional inhibitors targeting CDK9 and HDAC signaling pathways for cancer treatment. Among the synthesized compounds, 13ea demonstrated potent anti-proliferative activities (IC |
| title | Design, synthesis, and biological evaluation of N-(2-amino-phenyl)-5-(4-aryl- pyrimidin-2-yl) amino)-1H-indole-2-carboxamide derivatives as novel inhibitors of CDK9 and class I HDACs for cancer treatment. |
| topic | Humans Cyclin-Dependent Kinase 9 Histone Deacetylase Inhibitors Antineoplastic Agents Structure-Activity Relationship Drug Design Drug Screening Assays, Antitumor Cell Proliferation Molecular Structure Histone Deacetylases Indoles Dose-Response Relationship, Drug Animals Protein Kinase Inhibitors Mice Apoptosis Cell Line, Tumor Molecular Docking Simulation |
| url | https://pubmed.ncbi.nlm.nih.gov/40383016/ |