title: Synthesis and evaluation of in vitro antiproliferative activity of new ethyl 3-(arylethynyl)quinoxaline-2-carboxylate and pyrido[4,3-b]quinoxalin-1(2H)-one derivatives.
abstract: We report a novel series of quinoxaline derivatives from which agents with antiproliferative activity have been identified. Two ethyl 3-(arylethynyl)quinoxaline-2-carboxylates demonstrated substantial antiproliferative activity against both human non-small cell lung carcinoma (A549) and glioblastoma (U87-MG) cell lines. Pyrido[4,3-b]quinoxalin-1(2H)-ones demonstrated poor activity against A549 and U87-MG cell lines. Three of the derivatives in ethyl 3-(arylethynyl)quinoxaline-2-carboxylate series demonstrated substantial antiproliferative activity. The arylethynyl derivative 2a and 2d proved to be the most cytotoxic with an IC50value of 3.3 μM for both A549 and U87-MG cell lines.
authors: University of Carthage, Faculty of Sciences of Bizerte, Laboratory of Physics of Lamellaires Materials and Hybrids Nanomaterials, Zarzouna 7021, Bizerte, Tunisia.
authors: Majdi
authors: M
authors: Hajri
authors: Aix-Marseille Université, INSERM, CRO2, UMR_S911, 13385 Marseille, France; AP-HM, Hôpital Timone, Pharmacie, 13005 Marseille, France.
authors: Marie-Anne
authors: MA
authors: Esteve
authors: Aix-Marseille Université, CNRS, Institut de Chimie Radicalaire ICR, UMR 7273, Laboratoire de Pharmaco-Chimie Radicalaire, Marseille, France.
authors: Omar
authors: O
authors: Khoumeri
authors: University of Carthage, Faculty of Sciences of Bizerte, Laboratory of Physics of Lamellaires Materials and Hybrids Nanomaterials, Zarzouna 7021, Bizerte, Tunisia.
authors: Raoudha
authors: R
authors: Abderrahim
authors: Aix-Marseille Université, CNRS, Institut de Chimie Radicalaire ICR, UMR 7273, Laboratoire de Pharmaco-Chimie Radicalaire, Marseille, France.
authors: Thierry
authors: T
authors: Terme
authors: Aix-Marseille Université, CNRS, Institut de Chimie Radicalaire ICR, UMR 7273, Laboratoire de Pharmaco-Chimie Radicalaire, Marseille, France.
authors: Marc
authors: M
authors: Montana
authors: Aix-Marseille Université, CNRS, Institut de Chimie Radicalaire ICR, UMR 7273, Laboratoire de Pharmaco-Chimie Radicalaire, Marseille, France. Electronic address: patrice.vanelle@univ-amu.fr.
authors: Patrice
authors: P
authors: Vanelle
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D002264:Carboxylic Acids / Q000737:chemistry*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D060326:Chemistry Techniques, Synthetic; D015195:Drug Design; D006801:Humans; D011810:Quinoxalines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D002264:Carboxylic Acids; D011810:Quinoxalines
keywords: Antitumor activity; Organic chemistry; Quinoxaline; Structure-activity relationship