Optimization of pyrazole-containing 1,2,4-triazolo-[3,4-b]thiadiazines, a new class of STAT3 pathway inhibitors

Structure-activity relationship studies of a 1,2,4-triazolo-[3,4-b]thiadiazine scaffold, identified in an HTS campaign for selective STAT3 pathway inhibitors, determined that a pyrazole group and specific aryl substitution on the thiadiazine were necessary for activity. Improvements in potency and m...

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Détails bibliographiques
Publié dans:Bioorg Med Chem Lett
Auteurs principaux: LaPorte, Matthew G., Wang, Zhuzhu, Colombo, Raffaele, Garzan, Atefeh, Peshkov, Vsevolod A., Liang, Mary, Johnston, Paul A., Schurdak, Mark E., Sen, Malabika, Camarco, Daniel P., Hua, Yun, Pollock, Netanya I., Lazo, John S., Grandis, Jennifer R., Wipf, Peter, Huryn, Donna M.
Format: Artigo
Langue:Inglês
Publié: 2016
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Article
Accès en ligne:https://ncbi.nlm.nih.gov/pmc/articles/PMC4964800/
https://ncbi.nlm.nih.gov/pubmed/27381083
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2016.06.017
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