title: β-Nitro substituted carboxylic acids and their cytotoxicity.
abstract: β-Nitro-substituted ethyl carboxylates are a new class of cytotoxic agents; they can be easily obtained in fair to good yields in a single-step reaction by a Pd-catalyzed asymmetric conjugate addition of aryl boronic acids to 2-nitro-acrylates. Of all the tested derivatives, 2-(4-chlorophenyl)-3-nitropropionic acid ethyl ester (6) is most cytotoxic especially against the human ovarian cancer cell line A2780 therefore making this compound an interesting candidate for further investigations.
authors.affiliation: Martin-Luther Universität Halle-Wittenberg, Bereich Organische Chemie, Kurt-Mothes-Str. 2, D-06120 Halle (Saale), Germany. Electronic address: rene.csuk@chemie.uni-halle.de.
authors.forename: René
authors.initials: R
authors.lastname: Csuk
authors.affiliation: Martin-Luther Universität Halle-Wittenberg, Bereich Organische Chemie, Kurt-Mothes-Str. 2, D-06120 Halle (Saale), Germany.
authors.forename: Lucie
authors.initials: L
authors.lastname: Heller
authors.affiliation: Martin-Luther Universität Halle-Wittenberg, Bereich Organische Chemie, Kurt-Mothes-Str. 2, D-06120 Halle (Saale), Germany.
authors.forename: Bianka
authors.initials: B
authors.lastname: Siewert
authors.affiliation: Chiroblock GmbH, Andresenstr. 1a, D-06766 Bitterfeld-Wolfen, Germany.
authors.forename: Andrey
authors.initials: A
authors.lastname: Gutnov
authors.affiliation: Chiroblock GmbH, Andresenstr. 1a, D-06766 Bitterfeld-Wolfen, Germany.
authors.forename: Oliver
authors.initials: O
authors.lastname: Seidelmann
authors.affiliation: Chiroblock GmbH, Andresenstr. 1a, D-06766 Bitterfeld-Wolfen, Germany.
authors.forename: Volkmar
authors.initials: V
authors.lastname: Wendisch
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002264:Carboxylic Acids / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004353:Drug Evaluation, Preclinical; D005347:Fibroblasts / Q000187:drug effects; D006801:Humans; D061986:MCF-7 Cells; D051379:Mice; D015394:Molecular Structure; D041681:NIH 3T3 Cells; D009574:Nitro Compounds / Q000737:chemistry*; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D002264:Carboxylic Acids; D009574:Nitro Compounds
keywords: Cancer; Cytotoxicity; SRB assay; β-Nitro carboxylic acids