Autor segons l'article: 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.;
Departament: Química Analítica i Química Orgànica
Autor/s de la URV: BRAVO LARA, FERNANDO / ECHAVARREN PABLOS, ANTONIO
Paraules clau: Trpc4 Tonantzitlolone Pkc-theta Mice Kidney cancer Ion channels Formal synthesis Englerin Cytotoxicity Channels Biological evaluation (-)-englerin
Resum: 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.
Àrees temàtiques: 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
Accès a la llicència d'ús: https://creativecommons.org/licenses/by/3.0/es/
Adreça de correu electrònic de l'autor: antoniomaria.echavarren@urv.cat
Identificador de l'autor: 0000-0002-6418-7930
Data d'alta del registre: 2024-01-14
Versió de l'article dipositat: info:eu-repo/semantics/acceptedVersion
Enllaç font original: https://pubs.acs.org/doi/10.1021/acsmedchemlett.0c00186
Referència a l'article segons font original: Acs Medicinal Chemistry Letters. 11 (9): 1711-1716
Referència 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
URL Document de llicència: https://repositori.urv.cat/ca/proteccio-de-dades/
DOI de l'article: 10.1021/acsmedchemlett.0c00186
Entitat: Universitat Rovira i Virgili
Any de publicació de la revista: 2020
Tipus de publicació: Journal Publications
Repositori URV