{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"submitter":["Lu Z"],"funding":["National Natural Science Foundation of China"],"pagination":["696-703"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC8155281"],"repository":["biostudies-literature"],"omics_type":["Unknown"],"volume":["12(5)"],"pubmed_abstract":["We identified nitazoxanide (<b>NTZ</b>) 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 <b>NTZ</b>, and their STAT3 pathway inhibitory activities were found to be significantly correlated with their antiproliferative activities in HeLa cells. Derivatives <b>15</b> and <b>24</b> were observed to be more potent than the positive control <b>WP1066</b>, which is under phase I clinical trials. Compared with <b>NTZ</b>, <b>15</b> also exhibited much improved in vivo pharmacokinetic parameters in rats and efficacies against pr"],"journal":["ACS medicinal chemistry letters"],"pubmed_title":["Structure-Activity Study of Nitazoxanide Derivatives as Novel STAT3 Pathway Inhibitors."],"pmcid":["PMC8155281"],"funding_grant_id":["81872731","21977006"],"pubmed_authors":["Li X","Li C","Xu P","Du T","Wang C","Huang W","Lu Z","Xu F","Li K","Ji M","Niu Y"],"additional_accession":[]},"is_claimable":false,"name":"Structure-Activity Study of Nitazoxanide Derivatives as Novel STAT3 Pathway Inhibitors.","description":"We identified nitazoxanide (<b>NTZ</b>) 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 <b>NTZ</b>, and their STAT3 pathway inhibitory activities were found to be significantly correlated with their antiproliferative activities in HeLa cells. Derivatives <b>15</b> and <b>24</b> were observed to be more potent than the positive control <b>WP1066</b>, which is under phase I clinical trials. Compared with <b>NTZ</b>, <b>15</b> also exhibited much improved in vivo pharmacokinetic parameters in rats and efficacies against pr","dates":{"release":"2021-01-01T00:00:00Z","publication":"2021 May","modification":"2025-04-04T20:15:59.398Z","creation":"2025-04-04T20:15:59.398Z"},"accession":"S-EPMC8155281","cross_references":{"pubmed":["34055214"],"doi":["10.1021/acsmedchemlett.0c00544"]}}