{"title":"蛇床子醇三唑衍生物的合成、表征及细胞毒性评价","authors":"Zanib Hilal, Rishi Kant, Masood Nadeem, Saleem Farooq, Mushtaq Ahmad Tantray","doi":"10.1002/slct.202502327","DOIUrl":null,"url":null,"abstract":"<p>Osthol is a natural substance that has been shown to have a number of significant biological and pharmacological functions, most notably an inhibitory effect on several cancer types. Derivatization is an essential and fascinating area of research because of the unmet demands in cancer therapies. In light of this, a whole new range of varied osthol analogs was synthesized. All of these triazole derivatives were synthesized by altering the lactone ring of the osthol molecule at various positions. Cytotoxic potential was then tested against a urinary bladder cancer cell line (T24), for anticancer properties using MTT assay. Interestingly, among the tested molecules, most of the analogs displayed better anticancer activity than the parent osthol. However, compound T2 showed the highest efficacy against the bladder cell line out of all the investigated analogs, with an IC<sub>50</sub> of 52.6 mM in bladder cancer cells, with strong apoptotic effects and G1 phase arrest.</p>","PeriodicalId":146,"journal":{"name":"ChemistrySelect","volume":"10 32","pages":""},"PeriodicalIF":2.0000,"publicationDate":"2025-08-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Synthesis, Characterization, and Cytotoxicity Evaluation of Triazole Derivatives from Osthol\",\"authors\":\"Zanib Hilal, Rishi Kant, Masood Nadeem, Saleem Farooq, Mushtaq Ahmad Tantray\",\"doi\":\"10.1002/slct.202502327\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p>Osthol is a natural substance that has been shown to have a number of significant biological and pharmacological functions, most notably an inhibitory effect on several cancer types. Derivatization is an essential and fascinating area of research because of the unmet demands in cancer therapies. In light of this, a whole new range of varied osthol analogs was synthesized. All of these triazole derivatives were synthesized by altering the lactone ring of the osthol molecule at various positions. Cytotoxic potential was then tested against a urinary bladder cancer cell line (T24), for anticancer properties using MTT assay. Interestingly, among the tested molecules, most of the analogs displayed better anticancer activity than the parent osthol. However, compound T2 showed the highest efficacy against the bladder cell line out of all the investigated analogs, with an IC<sub>50</sub> of 52.6 mM in bladder cancer cells, with strong apoptotic effects and G1 phase arrest.</p>\",\"PeriodicalId\":146,\"journal\":{\"name\":\"ChemistrySelect\",\"volume\":\"10 32\",\"pages\":\"\"},\"PeriodicalIF\":2.0000,\"publicationDate\":\"2025-08-20\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"ChemistrySelect\",\"FirstCategoryId\":\"92\",\"ListUrlMain\":\"https://chemistry-europe.onlinelibrary.wiley.com/doi/10.1002/slct.202502327\",\"RegionNum\":4,\"RegionCategory\":\"化学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q3\",\"JCRName\":\"CHEMISTRY, MULTIDISCIPLINARY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"ChemistrySelect","FirstCategoryId":"92","ListUrlMain":"https://chemistry-europe.onlinelibrary.wiley.com/doi/10.1002/slct.202502327","RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"CHEMISTRY, MULTIDISCIPLINARY","Score":null,"Total":0}
Synthesis, Characterization, and Cytotoxicity Evaluation of Triazole Derivatives from Osthol
Osthol is a natural substance that has been shown to have a number of significant biological and pharmacological functions, most notably an inhibitory effect on several cancer types. Derivatization is an essential and fascinating area of research because of the unmet demands in cancer therapies. In light of this, a whole new range of varied osthol analogs was synthesized. All of these triazole derivatives were synthesized by altering the lactone ring of the osthol molecule at various positions. Cytotoxic potential was then tested against a urinary bladder cancer cell line (T24), for anticancer properties using MTT assay. Interestingly, among the tested molecules, most of the analogs displayed better anticancer activity than the parent osthol. However, compound T2 showed the highest efficacy against the bladder cell line out of all the investigated analogs, with an IC50 of 52.6 mM in bladder cancer cells, with strong apoptotic effects and G1 phase arrest.
期刊介绍:
ChemistrySelect is the latest journal from ChemPubSoc Europe and Wiley-VCH. It offers researchers a quality society-owned journal in which to publish their work in all areas of chemistry. Manuscripts are evaluated by active researchers to ensure they add meaningfully to the scientific literature, and those accepted are processed quickly to ensure rapid online publication.