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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Detalhes bibliográficos
Publicado no:Bioorg Med Chem Lett
Main Authors: 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.
Formato: Artigo
Idioma:Inglês
Publicado em: 2016
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Article
Acesso em linha: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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