{"title":"通过 1-arylpropynes 和腈的正规 [3+2] 环加成法合成 2,3,5-三取代的 1H 吡咯并提高其抗增殖活性","authors":"Dandan He, Ling Li, Xiong Wen, Luxiang Yin, Jue Li, Sha Wu, Huili Li, Fei Jiang, Xiangchun Shen","doi":"10.1039/d4qo01999g","DOIUrl":null,"url":null,"abstract":"A straightforward approach for the assemble of 2,3,5-trisubstituted 1H-pyrroles via a base-mediated [3+2] cycloaddition of 1-arylpropynes with nitriles has been reported through the alkali metal salts promoted C(sp3)-H functionalization. This reaction features transition metal-free catalyst, facile starting materials and wide substrate scope. Moreover, the biological evaluation revealed that these pyrrole products exhibit the antiproliferative activities of MDA-MB-231, SGC-7901, and HCT-116 cells, which provides a potential applications in pharmaceutical chemistry.","PeriodicalId":97,"journal":{"name":"Organic Chemistry Frontiers","volume":"3 1","pages":""},"PeriodicalIF":4.6000,"publicationDate":"2024-12-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Synthesis and antiproliferative activities of 2,3,5-trisubstituted 1H-pyrroles via formal [3+2] cycloaddition of 1-arylpropynes and nitriles\",\"authors\":\"Dandan He, Ling Li, Xiong Wen, Luxiang Yin, Jue Li, Sha Wu, Huili Li, Fei Jiang, Xiangchun Shen\",\"doi\":\"10.1039/d4qo01999g\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"A straightforward approach for the assemble of 2,3,5-trisubstituted 1H-pyrroles via a base-mediated [3+2] cycloaddition of 1-arylpropynes with nitriles has been reported through the alkali metal salts promoted C(sp3)-H functionalization. This reaction features transition metal-free catalyst, facile starting materials and wide substrate scope. Moreover, the biological evaluation revealed that these pyrrole products exhibit the antiproliferative activities of MDA-MB-231, SGC-7901, and HCT-116 cells, which provides a potential applications in pharmaceutical chemistry.\",\"PeriodicalId\":97,\"journal\":{\"name\":\"Organic Chemistry Frontiers\",\"volume\":\"3 1\",\"pages\":\"\"},\"PeriodicalIF\":4.6000,\"publicationDate\":\"2024-12-10\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Organic Chemistry Frontiers\",\"FirstCategoryId\":\"92\",\"ListUrlMain\":\"https://doi.org/10.1039/d4qo01999g\",\"RegionNum\":1,\"RegionCategory\":\"化学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q1\",\"JCRName\":\"CHEMISTRY, ORGANIC\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Organic Chemistry Frontiers","FirstCategoryId":"92","ListUrlMain":"https://doi.org/10.1039/d4qo01999g","RegionNum":1,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q1","JCRName":"CHEMISTRY, ORGANIC","Score":null,"Total":0}
Synthesis and antiproliferative activities of 2,3,5-trisubstituted 1H-pyrroles via formal [3+2] cycloaddition of 1-arylpropynes and nitriles
A straightforward approach for the assemble of 2,3,5-trisubstituted 1H-pyrroles via a base-mediated [3+2] cycloaddition of 1-arylpropynes with nitriles has been reported through the alkali metal salts promoted C(sp3)-H functionalization. This reaction features transition metal-free catalyst, facile starting materials and wide substrate scope. Moreover, the biological evaluation revealed that these pyrrole products exhibit the antiproliferative activities of MDA-MB-231, SGC-7901, and HCT-116 cells, which provides a potential applications in pharmaceutical chemistry.
期刊介绍:
Organic Chemistry Frontiers is an esteemed journal that publishes high-quality research across the field of organic chemistry. It places a significant emphasis on studies that contribute substantially to the field by introducing new or significantly improved protocols and methodologies. The journal covers a wide array of topics which include, but are not limited to, organic synthesis, the development of synthetic methodologies, catalysis, natural products, functional organic materials, supramolecular and macromolecular chemistry, as well as physical and computational organic chemistry.