期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 26, 期 15, 页码 3581-3585出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2016.06.017
关键词
STAT3 inhibitor; Triazolo-thiadiazines; Anti-cancer agents; STAT1
资金
- National Cancer Institute, National Institutes of Health [HSN261200800001E]
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 metabolic stability were accomplished by the introduction of an a-methyl group on the thiadiazine. Optimized compounds exhibited anti-proliferative activity, reduction of phosphorylated STAT3 levels and effects on STAT3 target genes. These compounds represent a starting point for further drug discovery efforts targeting the STAT3 pathway. (C) 2016 Elsevier Ltd. All rights reserved.
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