title: Synthesis and biological evaluation of novel 2-heteroarylimino-1,3-thiazolidin-4-ones as potential anti-tumor agents.
abstract: A series of 35 heteroarylimino-1,3-thiazolidinones with three sites of functionalization were synthesized and their antiproliferative properties were studied. The in vitro screening by MTT assay was performed against five cancer cell lines (human colon cancer cell lines HT29, HCT116 and SW620 and breast cancer cell lines MCF7 and MDA-MB-231). It was observed that N3-substituted thiazolidinones had moderate activities whereas 5-benzylidene thiazolidinones showed promising activities. To investigate the mechanism of action, detailed biological studies of six selected compounds (those presenting the lower mitotic index) were carried out on the human colon cancer HT29 cell line. Cell cycle assay revealed that those compounds induced cell accumulation in G2/M and in subG0/G1 phases of cell cycle. Moreover, dissipation of mitochondria membrane potential was observed as well as redox changes in treated cells.
authors.affiliation: Université de Lorraine, UMR CNRS 7565, Structure et Réactivité des Systèmes Moléculaires Complexes - Equipe 3 (HECRIN), 1 Boulevard Arago, 57070 Metz Technopôle, France.
authors.forename: Germain
authors.initials: G
authors.lastname: Revelant
authors.affiliation: Université de Lorraine, UMR CNRS 7565, Structure et Réactivité des Systèmes Moléculaires Complexes - Equipe 5 (2MIC), Campus Bridoux - rue du Général Delestraint, 57070 Metz Cedex, France.
authors.forename: Sophie
authors.initials: S
authors.lastname: Huber-Villaume
authors.affiliation: Université de Lorraine, UMR CNRS 7565, Structure et Réactivité des Systèmes Moléculaires Complexes - Equipe 3 (HECRIN), 1 Boulevard Arago, 57070 Metz Technopôle, France.
authors.forename: Sandrine
authors.initials: S
authors.lastname: Dunand
authors.affiliation: Université de Lorraine, UMR CNRS 7565, Structure et Réactivité des Systèmes Moléculaires Complexes - Equipe 3 (HECRIN), 1 Boulevard Arago, 57070 Metz Technopôle, France.
authors.forename: Gilbert
authors.initials: G
authors.lastname: Kirsch
authors.affiliation: Université de Lorraine, UMR CNRS 7565, Structure et Réactivité des Systèmes Moléculaires Complexes - Equipe 5 (2MIC), Campus Bridoux - rue du Général Delestraint, 57070 Metz Cedex, France. Electronic address: herve.schohn@univ-lorraine.fr.
authors.forename: Hervé
authors.initials: H
authors.lastname: Schohn
authors.affiliation: Université de Lorraine, UMR CNRS 7565, Structure et Réactivité des Systèmes Moléculaires Complexes - Equipe 3 (HECRIN), 1 Boulevard Arago, 57070 Metz Technopôle, France. Electronic address: stephanie.hesse@univ-lorraine.fr.
authors.forename: Stéphanie
authors.initials: S
authors.lastname: Hesse
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D001343:Autophagy / Q000187:drug effects; D002453:Cell Cycle / Q000187:drug effects; D045744:Cell Line, Tumor; D060326:Chemistry Techniques, Synthetic; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D020128:Inhibitory Concentration 50; D053078:Membrane Potential, Mitochondrial / Q000187:drug effects; D010084:Oxidation-Reduction; D013329:Structure-Activity Relationship; D053778:Thiazolidines / Q000737:chemistry
chemical_list: D000970:Antineoplastic Agents; D053778:Thiazolidines
keywords: Antiproliferative activity; Colon cancer; Thiazole; Thiazolidinone; Thiophene