title: Synthesis, reactivity and biological evaluation of novel halogenated tripentones.
abstract: We describe herein the synthesis and the biological evaluation of a novel series of a potent anticancer agents: the tripentones. For the first time, a halogen atom was introduced in high yields on the pyrrole ring of the tricycle. This synthesis and the reactivity of the novel halogenated tripentones in metallo-catalysed cross-coupling reactions will be described in that article. Finally their influence on biological activity will be discussed.
authors.affiliation: Centre d'Etudes et de Recherche sur le Médicament de Normandie (UPRES EA 4258-FR CNRS 3038 INC3M), UFR des Sciences Pharmaceutiques, Université de Caen Basse-Normandie, Boulevard Becquerel, 14032 Caen cedex, France.
authors.forename: Vittoria
authors.initials: V
authors.lastname: Perri
authors.forename: Christophe
authors.initials: C
authors.lastname: Rochais
authors.forename: Thierry
authors.initials: T
authors.lastname: Cresteil
authors.forename: Patrick
authors.initials: P
authors.lastname: Dallemagne
authors.forename: Sylvain
authors.initials: S
authors.lastname: Rault
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D003432:Cross-Linking Reagents / Q000737:chemistry; D004353:Drug Evaluation, Preclinical; D006801:Humans; D006846:Hydrocarbons, Halogenated / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D011763:Pyrrolizidine Alkaloids / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D003432:Cross-Linking Reagents; D006846:Hydrocarbons, Halogenated; D011763:Pyrrolizidine Alkaloids