Ontology highlight
ABSTRACT:
SUBMITTER: LaPorte MG
PROVIDER: S-EPMC4964800 | biostudies-literature | 2016 Aug
REPOSITORIES: biostudies-literature
Bioorganic & medicinal chemistry letters 20160609 15
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 α-methyl group on the thiadiazine. Optimized compounds exhibited anti-proliferative activity, reduction of phosphorylated STAT3 levels an ...[more]