title: A facile route to polysubstituted indoles via three-component reaction of 2-ethynylaniline, sulfonyl azide, and nitroolefin.
abstract: A copper-catalyzed three-component reaction of 2-ethynylaniline, sulfonyl azide, and nitroolefin is reported. This reaction generates functionalized indoles in good yields and proceeds smoothly under mild conditions. Some hits as an HCT-116 inhibitor are found from the preliminary biological screening.
authors.affiliation: Department of Chemistry, Fudan University, Shanghai, China.
authors.forename: Zhiyuan
authors.initials: Z
authors.lastname: Chen
authors.forename: Danqing
authors.initials: D
authors.lastname: Zheng
authors.forename: Jie
authors.initials: J
authors.lastname: Wu
mesh_terms: D000114:Acetylene / Q000031:analogs & derivatives* / Q000737:chemistry; D000475:Alkenes / Q000737:chemistry*; D000814:Aniline Compounds / Q000737:chemistry*; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001386:Azides / Q000737:chemistry*; D002384:Catalysis; D020650:Combinatorial Chemistry Techniques; D003300:Copper / Q000737:chemistry*; D004354:Drug Screening Assays, Antitumor; D045325:HCT116 Cells / Q000187:drug effects; D006801:Humans; D007211:Indoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D015394:Molecular Structure; D009574:Nitro Compounds / Q000737:chemistry*
chemical_list: C483919:2-ethynylaniline; D000475:Alkenes; D000814:Aniline Compounds; D000970:Antineoplastic Agents; D001386:Azides; D007211:Indoles; D009574:Nitro Compounds; D003300:Copper; D000114:Acetylene