{"title":"新型双-(三氟甲基-5-苯基-1,3,4-恶二唑-2-基)甲基)-1,8-萘啶支架的绿色合成及抗癌评价","authors":"Mahesh Ellanti (Conceptualization Data curation Validation Writing – review & editing) , Divya A (Software) , Kavati Shireesha (Visualization) , Kumara Swamy Jella (Supervision)","doi":"10.1080/00397911.2025.2501211","DOIUrl":null,"url":null,"abstract":"<div><div>Eco-friendly construction of a 3-(3,5-bis(trifluoromethyl)phenyl)-1-((5-phenyl-1,3,4-oxadiazol-2-yl) methyl)-1,8-naphthyridin-2(1H)-one derivatives (<strong>10a–j</strong>) under microwave method furnished excellent yields in minimal time with maximum selectivity in the presence of PhI(OAc)<sub>2</sub>. This route aligns with the principles of green chemistry due to its significantly reduced reaction time and enriched energy efficiency, simplicity, and high yields. The synthesized compounds were characterized by spectroscopic techniques IR,<sup>1</sup>H NMR,<sup>13</sup>C NMR, Mass spectrometry, and elemental analysis studies. All the synthesized compounds cytotoxicity was tested against four cancer cell lines, MCF-7, Colo-205, A549, and SiHa human Cervix cancer cell lines; all the compounds demonstrated remarkable <em>in vitro</em> anticancer activity, notably, among them, compound 10i exhibited the most potent anti-cancer activity of IC<sub>50</sub> valves are 11.21 ± 0.17 μM (MCF-7 breast cancer cell line), 11.62 ± 0.54 μM (Colo-205 colon cancer cell line), 17.85 ± 0.48 μM (A549 lung carcinoma epithelial cells), 19.64 ± 0.46 μM (SiHa human Cervix cancer cell line) compared with clinical standard drug.</div></div>","PeriodicalId":22119,"journal":{"name":"Synthetic Communications","volume":"55 11","pages":"Pages 815-824"},"PeriodicalIF":1.8000,"publicationDate":"2025-05-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Green synthesis and anticancer evaluation of novel bis-(trifluoromethyl-5-phenyl-1,3,4-oxadiazol-2-yl) methyl)-1,8-naphthyridine scaffolds\",\"authors\":\"Mahesh Ellanti (Conceptualization Data curation Validation Writing – review & editing) , Divya A (Software) , Kavati Shireesha (Visualization) , Kumara Swamy Jella (Supervision)\",\"doi\":\"10.1080/00397911.2025.2501211\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><div>Eco-friendly construction of a 3-(3,5-bis(trifluoromethyl)phenyl)-1-((5-phenyl-1,3,4-oxadiazol-2-yl) methyl)-1,8-naphthyridin-2(1H)-one derivatives (<strong>10a–j</strong>) under microwave method furnished excellent yields in minimal time with maximum selectivity in the presence of PhI(OAc)<sub>2</sub>. This route aligns with the principles of green chemistry due to its significantly reduced reaction time and enriched energy efficiency, simplicity, and high yields. The synthesized compounds were characterized by spectroscopic techniques IR,<sup>1</sup>H NMR,<sup>13</sup>C NMR, Mass spectrometry, and elemental analysis studies. All the synthesized compounds cytotoxicity was tested against four cancer cell lines, MCF-7, Colo-205, A549, and SiHa human Cervix cancer cell lines; all the compounds demonstrated remarkable <em>in vitro</em> anticancer activity, notably, among them, compound 10i exhibited the most potent anti-cancer activity of IC<sub>50</sub> valves are 11.21 ± 0.17 μM (MCF-7 breast cancer cell line), 11.62 ± 0.54 μM (Colo-205 colon cancer cell line), 17.85 ± 0.48 μM (A549 lung carcinoma epithelial cells), 19.64 ± 0.46 μM (SiHa human Cervix cancer cell line) compared with clinical standard drug.</div></div>\",\"PeriodicalId\":22119,\"journal\":{\"name\":\"Synthetic Communications\",\"volume\":\"55 11\",\"pages\":\"Pages 815-824\"},\"PeriodicalIF\":1.8000,\"publicationDate\":\"2025-05-12\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Synthetic Communications\",\"FirstCategoryId\":\"92\",\"ListUrlMain\":\"https://www.sciencedirect.com/org/science/article/pii/S0039791125000487\",\"RegionNum\":3,\"RegionCategory\":\"化学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q3\",\"JCRName\":\"CHEMISTRY, ORGANIC\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Synthetic Communications","FirstCategoryId":"92","ListUrlMain":"https://www.sciencedirect.com/org/science/article/pii/S0039791125000487","RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"CHEMISTRY, ORGANIC","Score":null,"Total":0}
Green synthesis and anticancer evaluation of novel bis-(trifluoromethyl-5-phenyl-1,3,4-oxadiazol-2-yl) methyl)-1,8-naphthyridine scaffolds
Eco-friendly construction of a 3-(3,5-bis(trifluoromethyl)phenyl)-1-((5-phenyl-1,3,4-oxadiazol-2-yl) methyl)-1,8-naphthyridin-2(1H)-one derivatives (10a–j) under microwave method furnished excellent yields in minimal time with maximum selectivity in the presence of PhI(OAc)2. This route aligns with the principles of green chemistry due to its significantly reduced reaction time and enriched energy efficiency, simplicity, and high yields. The synthesized compounds were characterized by spectroscopic techniques IR,1H NMR,13C NMR, Mass spectrometry, and elemental analysis studies. All the synthesized compounds cytotoxicity was tested against four cancer cell lines, MCF-7, Colo-205, A549, and SiHa human Cervix cancer cell lines; all the compounds demonstrated remarkable in vitro anticancer activity, notably, among them, compound 10i exhibited the most potent anti-cancer activity of IC50 valves are 11.21 ± 0.17 μM (MCF-7 breast cancer cell line), 11.62 ± 0.54 μM (Colo-205 colon cancer cell line), 17.85 ± 0.48 μM (A549 lung carcinoma epithelial cells), 19.64 ± 0.46 μM (SiHa human Cervix cancer cell line) compared with clinical standard drug.
期刊介绍:
Synthetic Communications presents communications describing new methods, reagents, and other synthetic work pertaining to organic chemistry with sufficient experimental detail to permit reported reactions to be repeated by a chemist reasonably skilled in the art. In addition, the Journal features short, focused review articles discussing topics within its remit of synthetic organic chemistry.