Kanghui Duan , Fuxing Tan , Hongming Xie , Haiwang Liu , Yingjun Zhang , Huanfeng Jiang , Wanqing Wu
{"title":"3,4,5-三取代异噁唑的设计、合成和抗肿瘤活性","authors":"Kanghui Duan , Fuxing Tan , Hongming Xie , Haiwang Liu , Yingjun Zhang , Huanfeng Jiang , Wanqing Wu","doi":"10.1016/j.ejmcr.2024.100203","DOIUrl":null,"url":null,"abstract":"<div><p>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 <strong>14</strong>–<strong>3</strong> has an IC<sub>50</sub> 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, <strong>14</strong>–<strong>3</strong> induces apoptosis and leads to cell cycle arrest in the G2/M phase. Cytotoxicity tests on human normal hepatocytes LO2 also demonstrates that <strong>14</strong>–<strong>3</strong> is less toxic than 5-Fu with no obvious toxicity. These results suggest that <strong>14</strong>–<strong>3</strong> is a potential candidate for the development of anti-tumor drugs.</p></div>","PeriodicalId":12015,"journal":{"name":"European Journal of Medicinal Chemistry Reports","volume":"12 ","pages":"Article 100203"},"PeriodicalIF":0.0000,"publicationDate":"2024-08-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S277241742400075X/pdfft?md5=d9d5bb3d63fdd470bae8fe1359c4c765&pid=1-s2.0-S277241742400075X-main.pdf","citationCount":"0","resultStr":"{\"title\":\"Design, synthesis and antitumor activity of 3,4,5-Trisubstituted Isoxazoles\",\"authors\":\"Kanghui Duan , Fuxing Tan , Hongming Xie , Haiwang Liu , Yingjun Zhang , Huanfeng Jiang , Wanqing Wu\",\"doi\":\"10.1016/j.ejmcr.2024.100203\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><p>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 <strong>14</strong>–<strong>3</strong> has an IC<sub>50</sub> 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, <strong>14</strong>–<strong>3</strong> induces apoptosis and leads to cell cycle arrest in the G2/M phase. Cytotoxicity tests on human normal hepatocytes LO2 also demonstrates that <strong>14</strong>–<strong>3</strong> is less toxic than 5-Fu with no obvious toxicity. These results suggest that <strong>14</strong>–<strong>3</strong> is a potential candidate for the development of anti-tumor drugs.</p></div>\",\"PeriodicalId\":12015,\"journal\":{\"name\":\"European Journal of Medicinal Chemistry Reports\",\"volume\":\"12 \",\"pages\":\"Article 100203\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2024-08-19\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://www.sciencedirect.com/science/article/pii/S277241742400075X/pdfft?md5=d9d5bb3d63fdd470bae8fe1359c4c765&pid=1-s2.0-S277241742400075X-main.pdf\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"European Journal of Medicinal Chemistry Reports\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://www.sciencedirect.com/science/article/pii/S277241742400075X\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"European Journal of Medicinal Chemistry Reports","FirstCategoryId":"1085","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S277241742400075X","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
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 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.
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