Synthesis, reactivity and biological evaluation of novel halogenated tripentones.
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.
Perri
Vittoria
V
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.
Rochais
Christophe
C
Cresteil
Thierry
T
Dallemagne
Patrick
P
Rault
Sylvain
S
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
D000970:Antineoplastic Agents; D003432:Cross-Linking Reagents; D006846:Hydrocarbons, Halogenated; D011763:Pyrrolizidine Alkaloids