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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書誌詳細
出版年:Bioorg Med Chem Lett
主要な著者: 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.
フォーマット: Artigo
言語:Inglês
出版事項: 2016
主題:
Article
オンライン･アクセス: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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