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Imidazopyridine-fused [1,3]diazepinones: modulations of positions 2 to 4 and their impacts on the anti-melanoma activity.
Baccon-Sollier, Paul Le; Malki, Yohan; Maye, Morgane; Ali, Lamiaa M A; Lichon, Laure; Cuq, Pierre; Vincent, Laure-Anaïs; Masurier, Nicolas.
Afiliación
  • Baccon-Sollier PL; Institut des Biomolécules Max Mousseron, UMR 5247, CNRS, Universités Montpellier, UFR des Sciences Pharmaceutiques et Biologiques, Montpellier, France.
  • Malki Y; Institut des Biomolécules Max Mousseron, UMR 5247, CNRS, Universités Montpellier, UFR des Sciences Pharmaceutiques et Biologiques, Montpellier, France.
  • Maye M; Institut des Biomolécules Max Mousseron, UMR 5247, CNRS, Universités Montpellier, UFR des Sciences Pharmaceutiques et Biologiques, Montpellier, France.
  • Ali LMA; Institut des Biomolécules Max Mousseron, UMR 5247, CNRS, Universités Montpellier, UFR des Sciences Pharmaceutiques et Biologiques, Montpellier, France.
  • Lichon L; Department of Biochemistry, Medical Research Institute, University of Alexandria, Alexandria, Egypt.
  • Cuq P; Institut des Biomolécules Max Mousseron, UMR 5247, CNRS, Universités Montpellier, UFR des Sciences Pharmaceutiques et Biologiques, Montpellier, France.
  • Vincent LA; Institut des Biomolécules Max Mousseron, UMR 5247, CNRS, Universités Montpellier, UFR des Sciences Pharmaceutiques et Biologiques, Montpellier, France.
  • Masurier N; Institut des Biomolécules Max Mousseron, UMR 5247, CNRS, Universités Montpellier, UFR des Sciences Pharmaceutiques et Biologiques, Montpellier, France.
J Enzyme Inhib Med Chem ; 35(1): 935-949, 2020 Dec.
Article en En | MEDLINE | ID: mdl-32249633
A series of 19 novel pyrido-imidazodiazepinones, with modulations of positions 2, 3 and 4 of the diazepine ring were synthesised and screened for their in vitro cytotoxic activities against two melanoma cell lines (A375 and MDA-MB-435) and for their potential toxicity against NIH-3T3 non-cancerous cells. Selected compounds were also evaluated on the NCI-60 cell line panel. The SAR study revealed that the molecular volume and the cLogP of compounds modified at position 2 were significantly correlated with the activity of these compounds on melanoma cell lines. Moreover, introduction of a heterocyclic group at position 2 or an azido-alkyl chain at position 4 led to compounds displaying a significantly different activity profile on the NCI-60 cell line panel, compared to phenyl-substituted compounds at position 2 of the diazepinone. This study provides us crucial information for the development of new derivatives active against melanoma.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Piridinas / Azepinas / Imidazoles / Melanoma / Antineoplásicos Límite: Animals / Humans Idioma: En Revista: J Enzyme Inhib Med Chem Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2020 Tipo del documento: Article País de afiliación: Francia Pais de publicación: Reino Unido
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Piridinas / Azepinas / Imidazoles / Melanoma / Antineoplásicos Límite: Animals / Humans Idioma: En Revista: J Enzyme Inhib Med Chem Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2020 Tipo del documento: Article País de afiliación: Francia Pais de publicación: Reino Unido