Structure-Activity Study of Nitazoxanide Derivatives as Novel STAT3 Pathway Inhibitors
We identified nitazoxanide (NTZ) as a moderate STAT3 pathway inhibitor through immunoblot analysis 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 positive control WP1066, which is under phase I clinical trials. Compared with NTZ, 15 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.
Broad-spectrum antibacterial benzamide compound and preparation method and application thereof
The invention provides a benzamide new compound with activity of resisting multiple bacteria anda preparation method and application thereof. The compound is 3, 4-dichloro-N-(5-nitrothiazole-2-yl) benzamide, the compound is small in molecular weight, rela
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Paragraph 0007; 0022
(2020/10/30)
Research on nitro-derivatives of biological interest. XVI. Structure-activity relationships as protozoocidal, anthelmintic and molluscicidal agents in 2-benzamido 5-nitrothiazole series
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Cavier,Gayral,Guillaumel,et al.
p. 539 - 543
(2007/10/07)
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