Design, synthesis and antitumor activity of 5-trifluoromethylpyrimidine derivatives as EGFR inhibitors
A new series of 5-trifluoromethylpyrimidine derivatives were designed and synthesised as EGFR inhibitors. Three tumour cells A549, MCF-7, PC-3 and EGFR kinase were employed to evaluate their biological activities. The results were shown that most of the target compounds existed excellent antitumor a...
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| Format: | Article |
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Taylor & Francis Group
2022-12-01
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| Series: | Journal of Enzyme Inhibition and Medicinal Chemistry |
| Subjects: | |
| Online Access: | https://www.tandfonline.com/doi/10.1080/14756366.2022.2128797 |
| _version_ | 1818016226572500992 |
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| author | Yaqing Zuo Rongrong Li Yan Zhang Guochen Bao Yi Le Longjia Yan |
| author_facet | Yaqing Zuo Rongrong Li Yan Zhang Guochen Bao Yi Le Longjia Yan |
| author_sort | Yaqing Zuo |
| collection | DOAJ |
| description | A new series of 5-trifluoromethylpyrimidine derivatives were designed and synthesised as EGFR inhibitors. Three tumour cells A549, MCF-7, PC-3 and EGFR kinase were employed to evaluate their biological activities. The results were shown that most of the target compounds existed excellent antitumor activities. In particular, the IC50 values of compound 9u (E)-3-((2-((4-(3-(3-fluorophenyl)acrylamido)phenyl)amino)-5-(trifluoromethyl)pyrimidin-4-yl)amino)-N-methylthiophene-2-carboxamide against A549, MCF-7, PC-3 cells and EGFR kinase reached to 0.35 μM, 3.24 μM, 5.12 μM, and 0.091 μM, respectively. Additionally, further researches revealed that compound 9u could induce early apoptosis of A549 cells and arrest the cells in G2/M phase. Taken together, these findings indicated that compound 9u was potential for developing as antitumor reagent. |
| first_indexed | 2024-04-14T07:09:03Z |
| format | Article |
| id | doaj.art-73071dcf92cd4afd9bd84c30769639ef |
| institution | Directory Open Access Journal |
| issn | 1475-6366 1475-6374 |
| language | English |
| last_indexed | 2024-04-14T07:09:03Z |
| publishDate | 2022-12-01 |
| publisher | Taylor & Francis Group |
| record_format | Article |
| series | Journal of Enzyme Inhibition and Medicinal Chemistry |
| spelling | doaj.art-73071dcf92cd4afd9bd84c30769639ef2022-12-22T02:06:28ZengTaylor & Francis GroupJournal of Enzyme Inhibition and Medicinal Chemistry1475-63661475-63742022-12-013712742275410.1080/14756366.2022.2128797Design, synthesis and antitumor activity of 5-trifluoromethylpyrimidine derivatives as EGFR inhibitorsYaqing Zuo0Rongrong Li1Yan Zhang2Guochen Bao3Yi Le4Longjia Yan5School of Pharmaceutical Sciences, Guizhou University, Guiyang, ChinaSchool of Pharmaceutical Sciences, Guizhou University, Guiyang, ChinaSchool of Pharmaceutical Sciences, Guizhou University, Guiyang, ChinaInstitute for Biomedical Materials and Devices (IBMD), Faculty of Science, University of Technology Sydney, Sydney, AustraliaSchool of Pharmaceutical Sciences, Guizhou University, Guiyang, ChinaSchool of Pharmaceutical Sciences, Guizhou University, Guiyang, ChinaA new series of 5-trifluoromethylpyrimidine derivatives were designed and synthesised as EGFR inhibitors. Three tumour cells A549, MCF-7, PC-3 and EGFR kinase were employed to evaluate their biological activities. The results were shown that most of the target compounds existed excellent antitumor activities. In particular, the IC50 values of compound 9u (E)-3-((2-((4-(3-(3-fluorophenyl)acrylamido)phenyl)amino)-5-(trifluoromethyl)pyrimidin-4-yl)amino)-N-methylthiophene-2-carboxamide against A549, MCF-7, PC-3 cells and EGFR kinase reached to 0.35 μM, 3.24 μM, 5.12 μM, and 0.091 μM, respectively. Additionally, further researches revealed that compound 9u could induce early apoptosis of A549 cells and arrest the cells in G2/M phase. Taken together, these findings indicated that compound 9u was potential for developing as antitumor reagent.https://www.tandfonline.com/doi/10.1080/14756366.2022.2128797EGFRinhibitorpyrimidineantitumorreagent |
| spellingShingle | Yaqing Zuo Rongrong Li Yan Zhang Guochen Bao Yi Le Longjia Yan Design, synthesis and antitumor activity of 5-trifluoromethylpyrimidine derivatives as EGFR inhibitors Journal of Enzyme Inhibition and Medicinal Chemistry EGFR inhibitor pyrimidine antitumor reagent |
| title | Design, synthesis and antitumor activity of 5-trifluoromethylpyrimidine derivatives as EGFR inhibitors |
| title_full | Design, synthesis and antitumor activity of 5-trifluoromethylpyrimidine derivatives as EGFR inhibitors |
| title_fullStr | Design, synthesis and antitumor activity of 5-trifluoromethylpyrimidine derivatives as EGFR inhibitors |
| title_full_unstemmed | Design, synthesis and antitumor activity of 5-trifluoromethylpyrimidine derivatives as EGFR inhibitors |
| title_short | Design, synthesis and antitumor activity of 5-trifluoromethylpyrimidine derivatives as EGFR inhibitors |
| title_sort | design synthesis and antitumor activity of 5 trifluoromethylpyrimidine derivatives as egfr inhibitors |
| topic | EGFR inhibitor pyrimidine antitumor reagent |
| url | https://www.tandfonline.com/doi/10.1080/14756366.2022.2128797 |
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