{"title":"Synthesis and in vitro antiproliferative evaluation of novel drimane oxepinyl triazoles from labdane diterpene sclareol","authors":"Gulzar Hussain, Manzoor Ahmed, Sundas Chowdhary, Sanket K. Shukla, Syed Khalid Yousuf","doi":"10.1007/s00044-024-03334-9","DOIUrl":null,"url":null,"abstract":"<div><p>A series of new oxepinyl triazoles were synthesized using labdane diterpene sclareol as a template. The synthesis process involved several steps including oxidation, oxetane ring opening, deacetylation, tosylation, and azidation followed by Huisgen’s 1,3-dipolar cycloaddition reaction with different alkynes. The newly synthesized compounds were confirmed using <sup>1</sup>H NMR and <sup>13</sup>C NMR. These novel drimane oxepinyl triazoles derived from labdane diterpene sclareol were evaluated for their antiproliferative efficacy in colon (HCT-116), breast (MCF-7), and lung (A-549) cancer cell lines. Compound <b>14m</b> demonstrated significant cytotoxic effects in all tested cell lines with an IC<sub>50</sub> of 16 µM. Initial investigations suggested that the compound induced apoptosis and inhibited cancer cell proliferation, indicating the potential of drimane oxepinyl triazoles as promising therapeutic agents for various cancers.</p></div>","PeriodicalId":699,"journal":{"name":"Medicinal Chemistry Research","volume":"34 1","pages":"240 - 251"},"PeriodicalIF":2.6000,"publicationDate":"2024-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Medicinal Chemistry Research","FirstCategoryId":"3","ListUrlMain":"https://link.springer.com/article/10.1007/s00044-024-03334-9","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"CHEMISTRY, MEDICINAL","Score":null,"Total":0}
引用次数: 0
Abstract
A series of new oxepinyl triazoles were synthesized using labdane diterpene sclareol as a template. The synthesis process involved several steps including oxidation, oxetane ring opening, deacetylation, tosylation, and azidation followed by Huisgen’s 1,3-dipolar cycloaddition reaction with different alkynes. The newly synthesized compounds were confirmed using 1H NMR and 13C NMR. These novel drimane oxepinyl triazoles derived from labdane diterpene sclareol were evaluated for their antiproliferative efficacy in colon (HCT-116), breast (MCF-7), and lung (A-549) cancer cell lines. Compound 14m demonstrated significant cytotoxic effects in all tested cell lines with an IC50 of 16 µM. Initial investigations suggested that the compound induced apoptosis and inhibited cancer cell proliferation, indicating the potential of drimane oxepinyl triazoles as promising therapeutic agents for various cancers.
期刊介绍：
Medicinal Chemistry Research (MCRE) publishes papers on a wide range of topics, favoring research with significant, new, and up-to-date information. Although the journal has a demanding peer review process, MCRE still boasts rapid publication, due in part, to the length of the submissions. The journal publishes significant research on various topics, many of which emphasize the structure-activity relationships of molecular biology.
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