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Synthesis and Biological Evaluation of New (-)-Englerin Analogues

  • Datos identificativos

    Identificador: PC:1455
    Autores:
    Antonio M.EchavarrenLaura López-SuárezLorena RiesgoFernando BravoTanya T. RansomJohn A. Beutler
    Resumen:
    We report the synthesis and biological evaluation of a series of (-)-englerinA analogues obtained along our previously reported synthetic route based on a stereoselective gold(I) cycloaddition process. This synthetic route is a convenient platform to access analogues with broad structural diversity and has led us to the discovery of unprecedented and easier-to-synthesize derivatives with an unsaturation in the cyclopentyl ring between C4 and C5. We also introduce novel analogues in which the original isopropyl motif has been substituted with cyclohexyl, phenyl, and cyclopropyl moieties. The high selectivity and growth-inhibitory activity shown by these new derivatives in renal cancer cell lines opens new ways toward the final goal of finding effective drugs for the treatment of renal cell carcinoma (RCC).
  • Otros:

    Autor según el artículo: Antonio M.Echavarren; Laura López-Suárez; Lorena Riesgo; Fernando Bravo; Tanya T. Ransom; John A. Beutler
    Departamento: Química Analítica i Química Orgànica
    Autor/es de la URV: ECHAVARREN PABLOS, ANTONIO MARIA; Laura López-Suárez; Lorena Riesgo; Fernando Bravo; Tanya T. Ransom; John A. Beutler
    Palabras clave: Enantioselective synthesis EnglerinA Gold catalysis
    Resumen: We report the synthesis and biological evaluation of a series of (-)-englerinA analogues obtained along our previously reported synthetic route based on a stereoselective gold(I) cycloaddition process. This synthetic route is a convenient platform to access analogues with broad structural diversity and has led us to the discovery of unprecedented and easier-to-synthesize derivatives with an unsaturation in the cyclopentyl ring between C4 and C5. We also introduce novel analogues in which the original isopropyl motif has been substituted with cyclohexyl, phenyl, and cyclopropyl moieties. The high selectivity and growth-inhibitory activity shown by these new derivatives in renal cancer cell lines opens new ways toward the final goal of finding effective drugs for the treatment of renal cell carcinoma (RCC).
    Áreas temáticas: Química Química Chemistry
    Acceso a la licencia de uso: https://creativecommons.org/licenses/by/3.0/es/
    ISSN: 1860-7179
    Identificador del autor: 0000-0001-6808-3007; n/a; 0000-0002-4389-6113; 0000-0001-5377-9829; 0000-0001-8922-8359; 0000-0002-4646-1924
    Fecha de alta del registro: 2016-04-19
    Versión del articulo depositado: info:eu-repo/semantics/acceptedVersion
    Enlace a la fuente original: https://chemistry-europe.onlinelibrary.wiley.com/doi/full/10.1002/cmdc.201600040
    URL Documento de licencia: https://repositori.urv.cat/ca/proteccio-de-dades/
    DOI del artículo: 10.1002/cmdc.201600040
    Entidad: Universitat Rovira i Virgili
    Año de publicación de la revista: 2016
    Tipo de publicación: Article Artículo Article
  • Palabras clave:

    Or -- Catàlisi
    Enantioselective synthesis
    EnglerinA
    Gold catalysis
    Química
    Química
    Chemistry
    1860-7179
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