Thiol-to-amine cyclization reaction enables screening of large libraries of macrocyclic compounds and the generation of sub-kilodalton ligands

Macrocyclic compounds are an attractive modality for drug development, but the limited availability of large, structurally diverse macrocyclic libraries hampers the discovery of leads. Here, we describe the discovery of efficient macrocyclization reactions based on thiol-to-amine ligations using bis...

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Detalles Bibliográficos
Autores principales: Kale, S. S., Bergeron-Brlek, M., Wu, Y., Kumar, M. G., Pham, M. V., Bortoli, J., Vesin, J., Kong, X.-D., Machado, J. Franco, Deyle, K., Gonschorek, P., Turcatti, G., Cendron, L., Angelini, A., Heinis, C.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Association for the Advancement of Science 2019
Materias:
Research Articles
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6703864/
https://www.ncbi.nlm.nih.gov/pubmed/31457083
http://dx.doi.org/10.1126/sciadv.aaw2851

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