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Design and characterization of a heterocyclic electrophilic fragment library for the discovery of cysteine-targeted covalent inhibitors

A fragment library of electrophilic small heterocycles was characterized through cysteine-reactivity and aqueous stability tests that suggested their potential as covalent warheads. The analysis of theoretical and experimental descriptors revealed correlations between the electronic properties of th...

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Detalles Bibliográficos
Autores principales: Keeley, A., Ábrányi-Balogh, P., Keserű, G. M.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Royal Society of Chemistry 2018
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6390469/
https://www.ncbi.nlm.nih.gov/pubmed/30881613
http://dx.doi.org/10.1039/c8md00327k