title: Synthesis and antiproliferative studies of 5-aryl-2-(3-thienylamino)-1,3,4-thiadiazoles.
abstract: A series of 5-aryl-2-(3-thienylamino)-1,3,4-thiadiazoles 3a-m were synthesized in good yields in two steps starting from thiophen-3-isothiocyanates. Those compounds as well as the thiosemicarbazide intermediates 2a-m were screened for their antiproliferative activity against a panel of six cancer cell lines. Among them, two 5-aryl-2-(3-thienylamino)-1,3,4-thiadiazoles (3f and 3i) have shown very interesting results with IC50 <10μM on three cell lines.
authors.affiliation: Université de Lorraine, Laboratoire de Synthèse et Réactivité des Systèmes Moléculaires Complexes UMR-SRSMC 7565, Equipe Hécrin, 1 boulevard Arago, 57070 Metz Technopôle, France.
authors.forename: Germain
authors.initials: G
authors.lastname: Revelant
authors.affiliation: Université de Lorraine, Laboratoire de Synthèse et Réactivité des Systèmes Moléculaires Complexes UMR-SRSMC 7565, Equipe Hécrin, 1 boulevard Arago, 57070 Metz Technopôle, France.
authors.forename: Charlène
authors.initials: C
authors.lastname: Gadais
authors.affiliation: Laboratoire de toxicologie, Université Libre de Bruxelles, Brussels, Belgium.
authors.forename: Véronique
authors.initials: V
authors.lastname: Mathieu
authors.affiliation: Université de Lorraine, Laboratoire de Synthèse et Réactivité des Systèmes Moléculaires Complexes UMR-SRSMC 7565, Equipe Hécrin, 1 boulevard Arago, 57070 Metz Technopôle, France.
authors.forename: Gilbert
authors.initials: G
authors.lastname: Kirsch
authors.affiliation: Université de Lorraine, Laboratoire de Synthèse et Réactivité des Systèmes Moléculaires Complexes UMR-SRSMC 7565, Equipe Hécrin, 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*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D020128:Inhibitory Concentration 50; D013830:Thiadiazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D013830:Thiadiazoles; C058949:1,3,4-thiadiazole
keywords: Antiproliferative agents; MTT assay; Thienylamino-1,3,4-thiadiazoles; Thienylisothiocyanates; Thienylthiosemicarbazides