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

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