Secondary Logo

Journal Logo

Institutional members access full text with Ovid®

The salicylanilide derivatives inhibit signal transducer and activator of transcription 3 pathways in A549 lung cancer cells

Hu, Minhuaa,*; Ye, Wenfengb,*; Li, Jiaminga; Zhou, Penga; Chu, Zhaoxinb; Huang, Weijuna

doi: 10.1097/CAD.0000000000000303
PRECLINICAL REPORTS
Buy

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.

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: ahtcm8888@sina.com

Received April 10, 2015

Accepted September 11, 2015

Copyright © 2016 Wolters Kluwer Health, Inc. All rights reserved.