Articles producció científica> Química Analítica i Química Orgànica

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

  • Dades identificatives

    Identificador: PC:1455
    Autors:
    Antonio M.EchavarrenLaura López-SuárezLorena RiesgoFernando BravoTanya T. RansomJohn A. Beutler
    Resum:
    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).
  • Altres:

    Autor segons l'article: Antonio M.Echavarren; Laura López-Suárez; Lorena Riesgo; Fernando Bravo; Tanya T. Ransom; John A. Beutler
    Departament: Química Analítica i Química Orgànica
    Autor/s de la URV: ECHAVARREN PABLOS, ANTONIO MARIA; Laura López-Suárez; Lorena Riesgo; Fernando Bravo; Tanya T. Ransom; John A. Beutler
    Paraules clau: Enantioselective synthesis EnglerinA Gold catalysis
    Resum: 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).
    Àrees temàtiques: Química Química Chemistry
    Accès a la llicència d'ús: https://creativecommons.org/licenses/by/3.0/es/
    ISSN: 1860-7179
    Identificador de l'autor: 0000-0001-6808-3007; n/a; 0000-0002-4389-6113; 0000-0001-5377-9829; 0000-0001-8922-8359; 0000-0002-4646-1924
    Data d'alta del registre: 2016-04-19
    Versió de l'article dipositat: info:eu-repo/semantics/acceptedVersion
    URL Document de llicència: https://repositori.urv.cat/ca/proteccio-de-dades/
    Entitat: Universitat Rovira i Virgili
    Any de publicació de la revista: 2016
    Tipus de publicació: Article Artículo Article
  • Paraules clau:

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

  • Cerca a google

    Search to google scholar