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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Vydáno v:Bioorg Med Chem Lett
Hlavní autoři: 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.
Médium: Artigo
Jazyk:Inglês
Vydáno: 2016
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Article
On-line přístup: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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