Design, synthesis and antitumor activity of 3,4,5-Trisubstituted Isoxazoles
In this study, 56 isoxazole derivatives were synthesized and their antitumor activity against 9 cancer cells, such as BXPC-3, MiaPaCa-2, PANC-1, MCF-7, HCT-116, HepG2, NCI-H460, A549 and B16 was detected. The results of pharmacological experiments indicated that most compounds exhibit good cytotoxic...
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| Format: | Article |
| Language: | English |
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Elsevier
2024-12-01
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| Series: | European Journal of Medicinal Chemistry Reports |
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| Online Access: | http://www.sciencedirect.com/science/article/pii/S277241742400075X |
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| author | Kanghui Duan Fuxing Tan Hongming Xie Haiwang Liu Yingjun Zhang Huanfeng Jiang Wanqing Wu |
| author_facet | Kanghui Duan Fuxing Tan Hongming Xie Haiwang Liu Yingjun Zhang Huanfeng Jiang Wanqing Wu |
| author_sort | Kanghui Duan |
| collection | DOAJ |
| description | In this study, 56 isoxazole derivatives were synthesized and their antitumor activity against 9 cancer cells, such as BXPC-3, MiaPaCa-2, PANC-1, MCF-7, HCT-116, HepG2, NCI-H460, A549 and B16 was detected. The results of pharmacological experiments indicated that most compounds exhibit good cytotoxicity against nine cancer cells. Among them, compound 14–3 has an IC50 of 2.4 μM for colon cancer cells HCT-116, which shows the best effect and is better than the broad-spectrum drug 5-Fluorouracil (5-Fu) for the treatment of colon cancer. In addition, 14–3 induces apoptosis and leads to cell cycle arrest in the G2/M phase. Cytotoxicity tests on human normal hepatocytes LO2 also demonstrates that 14–3 is less toxic than 5-Fu with no obvious toxicity. These results suggest that 14–3 is a potential candidate for the development of anti-tumor drugs. |
| format | Article |
| id | doaj-art-0adbbff9568d40c1bbc1e9fffb5099eb |
| institution | Kabale University |
| issn | 2772-4174 |
| language | English |
| publishDate | 2024-12-01 |
| publisher | Elsevier |
| record_format | Article |
| series | European Journal of Medicinal Chemistry Reports |
| spelling | doaj-art-0adbbff9568d40c1bbc1e9fffb5099eb2024-12-05T05:21:53ZengElsevierEuropean Journal of Medicinal Chemistry Reports2772-41742024-12-0112100203Design, synthesis and antitumor activity of 3,4,5-Trisubstituted IsoxazolesKanghui Duan0Fuxing Tan1Hongming Xie2Haiwang Liu3Yingjun Zhang4Huanfeng Jiang5Wanqing Wu6Key Laboratory of Functional Molecular Engineering of Guangdong Province, School of Chemistry and Chemical Engineering, South China University of Technology, Guangzhou, 510640, ChinaState Key Laboratory of Anti-Infective Drug Development, Sunshine Lake Pharma Company, Ltd., Dongguan, 523871, ChinaState Key Laboratory of Anti-Infective Drug Development, Sunshine Lake Pharma Company, Ltd., Dongguan, 523871, ChinaState Key Laboratory of Anti-Infective Drug Development, Sunshine Lake Pharma Company, Ltd., Dongguan, 523871, ChinaState Key Laboratory of Anti-Infective Drug Development, Sunshine Lake Pharma Company, Ltd., Dongguan, 523871, ChinaKey Laboratory of Functional Molecular Engineering of Guangdong Province, School of Chemistry and Chemical Engineering, South China University of Technology, Guangzhou, 510640, ChinaKey Laboratory of Functional Molecular Engineering of Guangdong Province, School of Chemistry and Chemical Engineering, South China University of Technology, Guangzhou, 510640, China; Corresponding author.In this study, 56 isoxazole derivatives were synthesized and their antitumor activity against 9 cancer cells, such as BXPC-3, MiaPaCa-2, PANC-1, MCF-7, HCT-116, HepG2, NCI-H460, A549 and B16 was detected. The results of pharmacological experiments indicated that most compounds exhibit good cytotoxicity against nine cancer cells. Among them, compound 14–3 has an IC50 of 2.4 μM for colon cancer cells HCT-116, which shows the best effect and is better than the broad-spectrum drug 5-Fluorouracil (5-Fu) for the treatment of colon cancer. In addition, 14–3 induces apoptosis and leads to cell cycle arrest in the G2/M phase. Cytotoxicity tests on human normal hepatocytes LO2 also demonstrates that 14–3 is less toxic than 5-Fu with no obvious toxicity. These results suggest that 14–3 is a potential candidate for the development of anti-tumor drugs.http://www.sciencedirect.com/science/article/pii/S277241742400075XIsoxazoleHCT-1165-FluorouracilAnti-tumor |
| spellingShingle | Kanghui Duan Fuxing Tan Hongming Xie Haiwang Liu Yingjun Zhang Huanfeng Jiang Wanqing Wu Design, synthesis and antitumor activity of 3,4,5-Trisubstituted Isoxazoles European Journal of Medicinal Chemistry Reports Isoxazole HCT-116 5-Fluorouracil Anti-tumor |
| title | Design, synthesis and antitumor activity of 3,4,5-Trisubstituted Isoxazoles |
| title_full | Design, synthesis and antitumor activity of 3,4,5-Trisubstituted Isoxazoles |
| title_fullStr | Design, synthesis and antitumor activity of 3,4,5-Trisubstituted Isoxazoles |
| title_full_unstemmed | Design, synthesis and antitumor activity of 3,4,5-Trisubstituted Isoxazoles |
| title_short | Design, synthesis and antitumor activity of 3,4,5-Trisubstituted Isoxazoles |
| title_sort | design synthesis and antitumor activity of 3 4 5 trisubstituted isoxazoles |
| topic | Isoxazole HCT-116 5-Fluorouracil Anti-tumor |
| url | http://www.sciencedirect.com/science/article/pii/S277241742400075X |
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