title: Synthesis of polysubstituted benzofuran derivatives as novel inhibitors of parasitic growth.
abstract: A series of polysubstituted benzofuran derivatives was easily and rapidly prepared using a tandem Sonogashira coupling/cyclization reaction. Subsequent acylation afforded a small library of 39 new compounds that were assayed in cellulo on Plasmodium falciparum and Trypanosoma brucei parasites. Some of them exhibited good inhibitory activity on T. brucei proliferation.
authors.affiliation: CNRS, Institut de Chimie des Substances Naturelles, UPR2301, Centre de Recherche de Gif, Avenue de la Terrasse, 91198 Gif-sur-Yvette Cedex, France.
authors.forename: Marion
authors.initials: M
authors.lastname: Thévenin
authors.forename: Sylviane
authors.initials: S
authors.lastname: Thoret
authors.forename: Philippe
authors.initials: P
authors.lastname: Grellier
authors.forename: Joëlle
authors.initials: J
authors.lastname: Dubois
mesh_terms: D000215:Acylation; D000981:Antiprotozoal Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001572:Benzofurans / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D003500:Cyclization; D021261:Parasitic Sensitivity Tests; D010963:Plasmodium falciparum / Q000187:drug effects; D013329:Structure-Activity Relationship; D014346:Trypanosoma brucei brucei / Q000187:drug effects
chemical_list: D000981:Antiprotozoal Agents; D001572:Benzofurans; C105430:benzofuran
keywords: Antiparasitic; Benzofurans; P. falciparum; Sonogashira coupling reaction; T. brucei