Natural product inspired optimization of a selective TRPV6 calcium channel inhibitor† †Electronic supplementary information (ESI) available: Tables S1–S3, Fig. S1–S4, protocols for FLIPR assays, confocal imaging and antiproliferative assays, preparation, crystal structure reports, HRMS results, 1H, 13C and 19F NMR spectra of all new compounds, and purity of final compounds. CCDC 1997201–1997205. For ESI and crystallographic data in CIF or other electronic format see DOI: 10.1039/d0md00145g

Autor: Rajesh Bhardwaj, Christoph Romanin, Jean-Louis Reymond, Aline Lucie Carrel, Roberto Parise-Filho, Micael Rodrigues Cunha, Matthias A. Hediger, Sonja Lindinger

Publikováno v: RSC Medicinal Chemistry
Rodrigues Cunha, Micael; Bhardwaj, Rajesh; Carrel, Aline Lucie; Lindinger, Sonja; Romanin, Christoph; Parise-Filho, Roberto; Hediger, Matthias A.; Reymond, Jean-Louis (2020). Natural product inspired optimization of a selective TRPV6 calcium channel inhibitor. RSC Medicinal Chemistry, 11(9), pp. 1032-1040. Royal Society of Chemistry 10.1039/D0MD00145G
Repositório Institucional da USP (Biblioteca Digital da Produção Intelectual)
Universidade de São Paulo (USP)
instacron:USP

Natural product derived analogues were surveyed, and an oxygenated analog was identified as a potent and selective TRPV6 inhibitor, with high microsomal stability and low off-target effects.
Transient receptor potential vanilloid 6 (TRPV6) is a

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::82f6e7af45859faee2026335ad3529ed
http://europepmc.org/articles/PMC7513592