{"title":"脂质二炔醇药物载体的氟化类似物:HCT116癌细胞的合成和细胞毒性","authors":"Pauline Rullièrea, François Lizeauxa, Etienne Jolyb, Stéphanie Ballereaua, Hafida Gasparda, Valérie Maravalc, Remi Chauvinc, Yves Génissona","doi":"10.17721/fujcv7i1p1-9","DOIUrl":null,"url":null,"abstract":"Lipidic alkynylcarbinols (LACs) have been identified as potential antitumor compounds, and a thorough understanding of their pharmacophoric environment is now required to elucidate their biological mode of action. In the dialkynylcarbinol (DAC) series, a specific study of the pharmacophore potential has been undertaken by focusing on the synthesis of three fluorinated derivatives followed by their biological evaluation. This work highlights the requirement of an electron-rich secondary carbinol center as a key structure for cytotoxicity in HCT116 cells.","PeriodicalId":42056,"journal":{"name":"French-Ukrainian Journal of Chemistry","volume":null,"pages":null},"PeriodicalIF":0.4000,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Fluorinated analogues of lipidic dialkynylcarbinol pharmacophores: synthesis and cytotoxicity in HCT116 cancer cells\",\"authors\":\"Pauline Rullièrea, François Lizeauxa, Etienne Jolyb, Stéphanie Ballereaua, Hafida Gasparda, Valérie Maravalc, Remi Chauvinc, Yves Génissona\",\"doi\":\"10.17721/fujcv7i1p1-9\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"Lipidic alkynylcarbinols (LACs) have been identified as potential antitumor compounds, and a thorough understanding of their pharmacophoric environment is now required to elucidate their biological mode of action. In the dialkynylcarbinol (DAC) series, a specific study of the pharmacophore potential has been undertaken by focusing on the synthesis of three fluorinated derivatives followed by their biological evaluation. This work highlights the requirement of an electron-rich secondary carbinol center as a key structure for cytotoxicity in HCT116 cells.\",\"PeriodicalId\":42056,\"journal\":{\"name\":\"French-Ukrainian Journal of Chemistry\",\"volume\":null,\"pages\":null},\"PeriodicalIF\":0.4000,\"publicationDate\":\"2019-01-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"French-Ukrainian Journal of Chemistry\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.17721/fujcv7i1p1-9\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q4\",\"JCRName\":\"CHEMISTRY, ANALYTICAL\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"French-Ukrainian Journal of Chemistry","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.17721/fujcv7i1p1-9","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q4","JCRName":"CHEMISTRY, ANALYTICAL","Score":null,"Total":0}
Fluorinated analogues of lipidic dialkynylcarbinol pharmacophores: synthesis and cytotoxicity in HCT116 cancer cells
Lipidic alkynylcarbinols (LACs) have been identified as potential antitumor compounds, and a thorough understanding of their pharmacophoric environment is now required to elucidate their biological mode of action. In the dialkynylcarbinol (DAC) series, a specific study of the pharmacophore potential has been undertaken by focusing on the synthesis of three fluorinated derivatives followed by their biological evaluation. This work highlights the requirement of an electron-rich secondary carbinol center as a key structure for cytotoxicity in HCT116 cells.
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