1. The salicylanilide derivatives inhibit signal transducer and activator of transcription 3 pathways in A549 lung cancer cells
- Author
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Wenfeng Ye, Hu Minhua, Jiaming Li, Huang Weijun, Zhaoxin Chu, and Peng Zhou
- Subjects
STAT3 Transcription Factor ,0301 basic medicine ,Cancer Research ,Transcription, Genetic ,Active Transport, Cell Nucleus ,Antineoplastic Agents ,Salicylanilides ,Stat3 Signaling Pathway ,03 medical and health sciences ,chemistry.chemical_compound ,Piperidines ,Cell Line, Tumor ,Salicylamides ,Humans ,Anilides ,Pharmacology (medical) ,Phosphorylation ,Phosphotyrosine ,STAT3 ,Cell Proliferation ,Cell Nucleus ,Pharmacology ,biology ,Janus Kinase 2 ,Salicylanilide ,030104 developmental biology ,Oncology ,chemistry ,Cell culture ,Benzamides ,Cancer cell ,STAT protein ,biology.protein ,Cancer research ,Signal transduction ,Signal Transduction - Abstract
The signal transducer and activator of transcription 3 (STAT3) is constitutively activated in certain cancer cells. Therefore, blocking the aberrant activity of STAT3 in tumor cells is a validated therapeutic strategy. To discover novel inhibitors of STAT3 activity, we report the salicylanilide derivatives as a new small molecule inhibitor of the STAT3 signaling pathway. The N-(3-chloro-4-fluorophenyl)-2-hydroxy-4-(3-(piperidin-1-yl)propoxy) benzamide potently inhibited the activation and transcriptional function of STAT3. These studies further validate STAT3 as a drug discovery target and provide evidence that pharmacological agents that can selectively reduce the phospho-STAT3 levels in human cancer cells result in tumor apoptosis and growth inhibition.
- Published
- 2016
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