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Enabling synthesis in fragment-based drug discovery by reactivity mapping: photoredox-mediated cross-dehydrogenative heteroarylation of cyclic amines

In fragment-based drug discovery (FBDD), a weakly binding fragment hit is elaborated into a potent ligand by bespoke functionalization along specific directions (growth vectors) from the fragment core in order to complement the 3D structure of the target protein. This structure-based design approach...

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Detalles Bibliográficos
Autores principales: Grainger, Rachel, Heightman, Tom D., Ley, Steven V., Lima, Fabio, Johnson, Christopher N.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Royal Society of Chemistry 2018
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6385880/
https://www.ncbi.nlm.nih.gov/pubmed/30881651
http://dx.doi.org/10.1039/c8sc04789h