M. Bu, Y. Zhang, S. Pan, M. Zhang, X. Guo, J. Wang
{"title":"新型桦木醇衍生物的设计、合成和抗癌活性评估","authors":"M. Bu, Y. Zhang, S. Pan, M. Zhang, X. Guo, J. Wang","doi":"10.1134/S1070363224110185","DOIUrl":null,"url":null,"abstract":"<p>A series of novel betulin-28-isatin hydrazone derivatives was prepared, which were evaluated for their anticancer activity. Among them, 3β-hydroxy-lup-20(29)-ene-28-[(5-bromo-1<i>H</i>-indole-2,3-dione)-3-yl]hydrazone exhibited the most potent anticancer activity against A549 cells, with an IC<sub>50</sub> value of 6.95 µM, being 3.85-fold more potent than its parental compound betulin. Meanwhile, it also exhibited a negligible anti-proliferative activity against the human normal GES-1 cells, indicating its significant selectivity in inhibiting the proliferation of cancer cells than normal cells. The further virtual screening and mechanism studies suggested that this compound exerts its anticancer activity through the inhibition of PI3K-Akt signaling pathway. In summary, 3β-hydroxy-lup-20(29)-ene-28-[(5-bromo-1<i>H</i>-indole-2,3-dione)-3-yl]hydrazone can be used as a valuable skeleton for developing novel anticancer agents.</p>","PeriodicalId":761,"journal":{"name":"Russian Journal of General Chemistry","volume":"94 11","pages":"2957 - 2966"},"PeriodicalIF":0.9000,"publicationDate":"2024-12-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Design, Synthesis, and Anticancer Activity Evaluation of Novel Betulin Derivatives\",\"authors\":\"M. Bu, Y. Zhang, S. Pan, M. Zhang, X. Guo, J. Wang\",\"doi\":\"10.1134/S1070363224110185\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p>A series of novel betulin-28-isatin hydrazone derivatives was prepared, which were evaluated for their anticancer activity. Among them, 3β-hydroxy-lup-20(29)-ene-28-[(5-bromo-1<i>H</i>-indole-2,3-dione)-3-yl]hydrazone exhibited the most potent anticancer activity against A549 cells, with an IC<sub>50</sub> value of 6.95 µM, being 3.85-fold more potent than its parental compound betulin. Meanwhile, it also exhibited a negligible anti-proliferative activity against the human normal GES-1 cells, indicating its significant selectivity in inhibiting the proliferation of cancer cells than normal cells. The further virtual screening and mechanism studies suggested that this compound exerts its anticancer activity through the inhibition of PI3K-Akt signaling pathway. In summary, 3β-hydroxy-lup-20(29)-ene-28-[(5-bromo-1<i>H</i>-indole-2,3-dione)-3-yl]hydrazone can be used as a valuable skeleton for developing novel anticancer agents.</p>\",\"PeriodicalId\":761,\"journal\":{\"name\":\"Russian Journal of General Chemistry\",\"volume\":\"94 11\",\"pages\":\"2957 - 2966\"},\"PeriodicalIF\":0.9000,\"publicationDate\":\"2024-12-17\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Russian Journal of General Chemistry\",\"FirstCategoryId\":\"92\",\"ListUrlMain\":\"https://link.springer.com/article/10.1134/S1070363224110185\",\"RegionNum\":4,\"RegionCategory\":\"化学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q4\",\"JCRName\":\"CHEMISTRY, MULTIDISCIPLINARY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Russian Journal of General Chemistry","FirstCategoryId":"92","ListUrlMain":"https://link.springer.com/article/10.1134/S1070363224110185","RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q4","JCRName":"CHEMISTRY, MULTIDISCIPLINARY","Score":null,"Total":0}
Design, Synthesis, and Anticancer Activity Evaluation of Novel Betulin Derivatives
A series of novel betulin-28-isatin hydrazone derivatives was prepared, which were evaluated for their anticancer activity. Among them, 3β-hydroxy-lup-20(29)-ene-28-[(5-bromo-1H-indole-2,3-dione)-3-yl]hydrazone exhibited the most potent anticancer activity against A549 cells, with an IC50 value of 6.95 µM, being 3.85-fold more potent than its parental compound betulin. Meanwhile, it also exhibited a negligible anti-proliferative activity against the human normal GES-1 cells, indicating its significant selectivity in inhibiting the proliferation of cancer cells than normal cells. The further virtual screening and mechanism studies suggested that this compound exerts its anticancer activity through the inhibition of PI3K-Akt signaling pathway. In summary, 3β-hydroxy-lup-20(29)-ene-28-[(5-bromo-1H-indole-2,3-dione)-3-yl]hydrazone can be used as a valuable skeleton for developing novel anticancer agents.
期刊介绍：
Russian Journal of General Chemistry is a journal that covers many problems that are of general interest to the whole community of chemists. The journal is the successor to Russia’s first chemical journal, Zhurnal Russkogo Khimicheskogo Obshchestva (Journal of the Russian Chemical Society ) founded in 1869 to cover all aspects of chemistry. Now the journal is focused on the interdisciplinary areas of chemistry (organometallics, organometalloids, organoinorganic complexes, mechanochemistry, nanochemistry, etc.), new achievements and long-term results in the field. The journal publishes reviews, current scientific papers, letters to the editor, and discussion papers.
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