Autor segons l'article: López-Suárez L; Riesgo L; Bravo F; Ransom T; Beutler J; Echavarren A
Departament: Química Analítica i Química Orgànica
Autor/s de la URV: ECHAVARREN PABLOS, ANTONIO
Paraules clau: Tumor growth inhibition Renal cancer Natural products Gold catalysis Englerin a Enantioselective synthesis
Resum: © 2016 The Authors. We report the synthesis and biological evaluation of a series of (-)-englerin A 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: Saúde coletiva Química Pharmacology, toxicology and pharmaceutics (miscellaneous) Pharmacology, toxicology and pharmaceutics (all) Pharmacology & pharmacy Pharmacology Organic chemistry Odontología Molecular medicine Medicina ii Medicina i Materiais Interdisciplinar General pharmacology, toxicology and pharmaceutics General medicine Farmacia Drug discovery Ciências biológicas iii Ciências biológicas ii Ciências biológicas i Ciências ambientais 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: 2024-10-26
Versió de l'article dipositat: info:eu-repo/semantics/publishedVersion
Referència a l'article segons font original: Chemmedchem. 11 (9): 1003-1007
Referència de l'ítem segons les normes APA: López-Suárez L; Riesgo L; Bravo F; Ransom T; Beutler J; Echavarren A (2016). Synthesis and Biological Evaluation of New (-)-Englerin Analogues. Chemmedchem, 11(9), 1003-1007. DOI: 10.1002/cmdc.201600040
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: Journal Publications
Repositori URV