Autor según el artículo: Wu, Zhenhua; Suppo, Jean-Simon; Tumova, Sarka; Strope, Jonathan; Bravo, Fernando; Moy, Melody; Weinstein, Ethan S.; Peer, Cody J.; Figg, William D.; Chain, William J.; Echavarren, Antonio M.; Beech, David J.; Beutler, John A.;
Departamento: Química Analítica i Química Orgànica
Autor/es de la URV: BRAVO LARA, FERNANDO / ECHAVARREN PABLOS, ANTONIO
Palabras clave: Trpc4 Tonantzitlolone Pkc-theta Mice Kidney cancer Ion channels Formal synthesis Englerin Cytotoxicity Channels Biological evaluation (-)-englerin
Resumen: Modifications at the bridgehead position of englerin A were made to explore the effects of variation at this site on the molecule for biological activity, as judged by the NCI 60 screen, in which englerin A is highly potent and selective for renal cancer cells. Replacement of the isopropyl group by other, larger substituents yielded compounds which displayed excellent selectivity and potency comparable to the natural product. Selected compounds were also evaluated for their effect on the ion channel TRPC4 as well as for intravenous toxicity in mice, and these had lower potency in both assays compared to englerin A.
Áreas temáticas: Química Organic chemistry Medicina ii Medicina i Materiais Interdisciplinar Farmacia Drug discovery Ciências biológicas iii Ciências biológicas ii Ciências biológicas i Chemistry, medicinal Biotecnología Biochemistry
Acceso a la licencia de uso: https://creativecommons.org/licenses/by/3.0/es/
Direcció de correo del autor: antoniomaria.echavarren@urv.cat
Identificador del autor: 0000-0002-6418-7930
Fecha de alta del registro: 2024-01-14
Versión del articulo depositado: info:eu-repo/semantics/acceptedVersion
Enlace a la fuente original: https://pubs.acs.org/doi/10.1021/acsmedchemlett.0c00186
URL Documento de licencia: http://repositori.urv.cat/ca/proteccio-de-dades/
Referencia al articulo segun fuente origial: Acs Medicinal Chemistry Letters. 11 (9): 1711-1716
Referencia de l'ítem segons les normes APA: Wu, Zhenhua; Suppo, Jean-Simon; Tumova, Sarka; Strope, Jonathan; Bravo, Fernando; Moy, Melody; Weinstein, Ethan S.; Peer, Cody J.; Figg, William D.; C (2020). Bridgehead Modifications of Englerin A Reduce TRPC4 Activity and Intravenous Toxicity but not Cell Growth Inhibition. Acs Medicinal Chemistry Letters, 11(9), 1711-1716. DOI: 10.1021/acsmedchemlett.0c00186
DOI del artículo: 10.1021/acsmedchemlett.0c00186
Entidad: Universitat Rovira i Virgili
Año de publicación de la revista: 2020
Tipo de publicación: Journal Publications
Repositori URV