Lu, Zirui published the artcileStructure-Activity Study of Nitazoxanide Derivatives as Novel STAT3 Pathway Inhibitors, Quality Control of 55981-09-4, the main research area is thiazolides nitazoxanide antitumor STAT3 pathway inhibitor.
We identified nitazoxanide (NTZ) as a moderate STAT3 pathway inhibitor through immunoblot anal. and a cell-based IL-6/JAK/STAT3 pathway activation assay. A series of thiazolide derivatives were designed and synthesized to further validate the thiazolide scaffold as STAT3 inhibitors. Eight out of 25 derivatives displayed potencies greater than that of NTZ, and their STAT3 pathway inhibitory activities were found to be significantly correlated with their antiproliferative activities in HeLa cells. Derivatives 15 and 24 were observed to be more potent than the pos. control WP1066, which is under phase I clin. trials. Compared with NTZ, 15(I) also exhibited much improved in vivo pharmacokinetic parameters in rats and efficacies against proliferations in multiple cancer cell lines, indicating a broad-spectrum effect of these thiazolides as antitumor agents targeted on STAT3.
ACS Medicinal Chemistry Letters published new progress about Antitumor agents. 55981-09-4 belongs to class esters-buliding-blocks, name is 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, and the molecular formula is C12H9N3O5S, Quality Control of 55981-09-4.
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