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The Effect of Core Replacement on S64315, a Selective MCL-1 Inhibitor, and Its Analogues

[Image: see text] Following the identification of thieno[2,3-d]pyrimidine-based selective and potent inhibitors of MCL-1, we explored the effect of core swapping at different levels of advancement. During hit-to-lead optimization, X-ray-guided S-N replacement in the core provided a new vector, whose...

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Detalles Bibliográficos
Autores principales: Sipos, Szabolcs, Bálint, Balázs, Szabó, Zoltán B., Ondi, Levente, Csékei, Márton, Szlávik, Zoltán, Proszenyák, Ágnes, Murray, James B., Davidson, James, Chen, Ijen, Dokurno, Pawel, Surgenor, Allan E., Pedder, Christopher, Hubbard, Roderick E., Maragno, Ana-Leticia, Chanrion, Maia, Colland, Frederic, Geneste, Olivier, Kotschy, András
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2021
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8412899/
https://www.ncbi.nlm.nih.gov/pubmed/34497901
http://dx.doi.org/10.1021/acsomega.1c02595