{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"submitter":["Ravish A"],"funding":["National Research Foundation of Korea (NRF)","DBT-NER, and Vision Group on Science and Technology (CESEM), Government of Karnataka","Shenzhen Key Laboratory of Innovative Oncotherapeutics","Researchers Supporting Project","Overseas Research Cooperation Project","Shenzhen Development and Reform Commission Subject Construction Project","Tsinghua University Stable Funding Key Project","Shenzhen Bay Laboratory"],"pagination":["159"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC9952374"],"repository":["biostudies-literature"],"omics_type":["Unknown"],"volume":["10(2)"],"pubmed_abstract":["In breast cancer (BC), STAT3 is hyperactivated. This study explored the design of imidazopyridine-tethered pyrazolines as a de novo drug strategy for inhibiting STAT3 phosphorylation in human BC cells. This involved the synthesis and characterization of two series of compounds namely, 1-(3-(2,6-dimethylimidazo [1,2-a]pyridin-3-yl)-5-(3-nitrophenyl)-4,5-dihydro-1H-pyrazol-1-yl)-2-(4-(substituted)piperazin-1-yl)ethanone and N-substituted-3-(2,6-dimethylimidazo[1,2-a]pyridin-3-yl)-5-(3-nitrophenyl)-4,5-dihydro-1H-pyrazoline-1-carbothioamides. Compound <b>3f</b> with 2,3-dichlorophenyl substitution was recognized among the tested series as a lead structure that inhibited the viability of MCF-7 cells with an IC<sub>50</sub> value of 9.2 μM. A dose- and time-dependent inhibition of STAT3 phospho"],"journal":["Bioengineering (Basel, Switzerland)"],"pubmed_title":["De Novo Design of Imidazopyridine-Tethered Pyrazolines That Target Phosphorylation of STAT3 in Human Breast Cancer Cells."],"pmcid":["PMC9952374"],"funding_grant_id":["[2017]1434","HW2020008","NRF-2021R1I1A2060024","21310031","RSP2023R5","WDZC20200821150704001","ZDSYS20200820165400003"],"pubmed_authors":["Alharbi SA","Xi Z","Lobie PE","Yang JR","Shivakumar R","Chinnathambi A","Ravish A","Swamynayaka A","Pandey V","Basappa B","Madegowda M","Yang MH","Ahn KS","Nagaraja O","Sethi G"],"additional_accession":[]},"is_claimable":false,"name":"De Novo Design of Imidazopyridine-Tethered Pyrazolines That Target Phosphorylation of STAT3 in Human Breast Cancer Cells.","description":"In breast cancer (BC), STAT3 is hyperactivated. This study explored the design of imidazopyridine-tethered pyrazolines as a de novo drug strategy for inhibiting STAT3 phosphorylation in human BC cells. This involved the synthesis and characterization of two series of compounds namely, 1-(3-(2,6-dimethylimidazo [1,2-a]pyridin-3-yl)-5-(3-nitrophenyl)-4,5-dihydro-1H-pyrazol-1-yl)-2-(4-(substituted)piperazin-1-yl)ethanone and N-substituted-3-(2,6-dimethylimidazo[1,2-a]pyridin-3-yl)-5-(3-nitrophenyl)-4,5-dihydro-1H-pyrazoline-1-carbothioamides. Compound <b>3f</b> with 2,3-dichlorophenyl substitution was recognized among the tested series as a lead structure that inhibited the viability of MCF-7 cells with an IC<sub>50</sub> value of 9.2 μM. A dose- and time-dependent inhibition of STAT3 phospho","dates":{"release":"2023-01-01T00:00:00Z","publication":"2023 Jan","modification":"2026-04-08T13:21:42.807Z","creation":"2025-02-19T00:14:00.673Z"},"accession":"S-EPMC9952374","cross_references":{"pubmed":["36829653"],"doi":["10.3390/bioengineering10020159"]}}