Synthesis and biological evaluation of new dipyrrolo[3,4-a:3,4-c]carbazole-1,3,4,6-tetraones, substituted with various saturated and unsaturated side chains via palladium catalyzed cross-coupling reactions

Hélène Henon (1) , Fabrice Anizon (1) , Roy Golsteyn , Stéphane Leonce , Robert Hofmann , Bruno Pfeiffer , Michelle Prudhomme (1)

1 SEESIB - Synthèse et étude de systèmes à intêret biologique

The syntheses of a series of dipyrrolo[3,4-a:3,4-c]carbazole-1,3,4,6-tetraones, substituted in 10-position with saturated and unsaturated side chains, via palladium catalyzed cross-coupling reactions, are described. These compounds can be considered as granulatimide bis-imide analogues. Their inhibitory activity toward Chk1 kinase and their antiproliferative activities in vitro in four tumor cell lines are reported

Mots clés: Isogranulatimide; Antitumor agents; Dipyrrolo[3; 4-a:3; 4-c]carbazole-1; 6-tetraone; Chk1 inhibitors

Domaines: Chimie thérapeutique

Hélène Henon, Fabrice Anizon, Roy Golsteyn, Stéphane Leonce, Robert Hofmann, et al.. Synthesis and biological evaluation of new dipyrrolo[3,4-a:3,4-c]carbazole-1,3,4,6-tetraones, substituted with various saturated and unsaturated side chains via palladium catalyzed cross-coupling reactions. Bioorganic and Medicinal Chemistry, 2006, 14, pp.3825-3834. ⟨10.1016/j.bmc.2006.01.030⟩. ⟨hal-00023499⟩