title: 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.
abstract: 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.
authors.affiliation: Laboratoire SEESIB, Université Blaise Pascal, UMR 6504 du CNRS, 63177 Aubière, France.
authors.forename: Hélène
authors.initials: H
authors.lastname: Hénon
authors.forename: Fabrice
authors.initials: F
authors.lastname: Anizon
authors.forename: Roy M
authors.initials: RM
authors.lastname: Golsteyn
authors.forename: Stéphane
authors.initials: S
authors.lastname: Léonce
authors.forename: Robert
authors.initials: R
authors.lastname: Hofmann
authors.forename: Bruno
authors.initials: B
authors.lastname: Pfeiffer
authors.forename: Michelle
authors.initials: M
authors.lastname: Prudhomme
mesh_terms: D000818:Animals; D002227:Carbazoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D002384:Catalysis; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D000071877:Checkpoint Kinase 1; D003500:Cyclization; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D066298:In Vitro Techniques; D015394:Molecular Structure; D010165:Palladium / Q000737:chemistry*; D011494:Protein Kinases / Q000187:drug effects; D011758:Pyrroles / Q000138:chemical synthesis* / Q000494:pharmacology*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D002227:Carbazoles; D011758:Pyrroles; C512323:dipyrrolo(3,4-a:3,4-c)carbazole-1,3,4,6-tetraone; D010165:Palladium; D011494:Protein Kinases; C000605867:CHEK1 protein, human; D000071877:Checkpoint Kinase 1