Author, as appears in the article.: Antonio M.Echavarren; Laura López-Suárez; Lorena Riesgo; Fernando Bravo; Tanya T. Ransom; John A. Beutler
Department: Química Analítica i Química Orgànica
URV's Author/s: ECHAVARREN PABLOS, ANTONIO MARIA; Laura López-Suárez; Lorena Riesgo; Fernando Bravo; Tanya T. Ransom; John A. Beutler
Keywords: Enantioselective synthesis EnglerinA Gold catalysis
Abstract: 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).
Thematic Areas: Química Química Chemistry
licence for use: https://creativecommons.org/licenses/by/3.0/es/
ISSN: 1860-7179
Author identifier: 0000-0001-6808-3007; n/a; 0000-0002-4389-6113; 0000-0001-5377-9829; 0000-0001-8922-8359; 0000-0002-4646-1924
Record's date: 2016-04-19
Papper version: info:eu-repo/semantics/acceptedVersion
Link to the original source: https://chemistry-europe.onlinelibrary.wiley.com/doi/full/10.1002/cmdc.201600040
Licence document URL: https://repositori.urv.cat/ca/proteccio-de-dades/
Article's DOI: 10.1002/cmdc.201600040
Entity: Universitat Rovira i Virgili
Journal publication year: 2016
Publication Type: Article Artículo Article
Repositori URV