PRECLINICAL REPORTSThe salicylanilide derivatives inhibit signal transducer and activator of transcription 3 pathways in A549 lung cancer cellsHu, Minhuaa,*; Ye, Wenfengb,*; Li, Jiaminga; Zhou, Penga; Chu, Zhaoxinb; Huang, WeijunaAuthor Information aDepartment of Pharmaceutical Chemistry, Anhui University of Chinese Medicine bHefei Medical Engineering Pharmaceutical Co. Ltd, Hefei, People’s Republic of China * Minhua Hu and Wenfeng Ye contributed equally to the writing of this article. Correspondence to Jiaming Li, PhD, Department of Pharmaceutical Chemistry, Anhui University of Chinese Medicine, Hefei 230031, People’s Republic of China Tel: +86 13705 694971; e-mail: [email protected] Received April 10, 2015 Accepted September 11, 2015 Anti-Cancer Drugs: January 2016 - Volume 27 - Issue 1 - p 41-47 doi: 10.1097/CAD.0000000000000303 Buy Metrics 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. Copyright © 2016 Wolters Kluwer Health, Inc. All rights reserved.