Design, synthesis and evaluation of XZH-5 analogues as STAT3 inhibitors

被引：12

作者：

Daka, Philias ^{[1
]}

Liu, Aiguo ^{[2
]}

Karunaratne, Chamini ^{[1
]}

Csatary, Erika ^{[1
]}

Williams, Cameron ^{[1
]}

Xiao, Hui ^{[3
,4
]}

Lin, Jiayuh ^{[3
,4
]}

Xu, Zhenghu ^{[5
]}

Page, Richard C. ^{[1
]}

Wang, Hong ^{[1
]}

机构：

[1] Miami Univ, Dept Chem & Biochem, Oxford, OH 45056 USA

[2] Huazhong Univ Sci & Technol, Tongji Med Coll, Dept Pediat, Wuhan 430030, Hubei Province, Peoples R China

[3] Ohio State Univ, Dept Pediat, Nationwide Childrens Hosp, Ctr Childhood Canc & Blood Dis,Res Inst, Columbus, OH 43210 USA

[4] Ohio State Univ, Mol Cellular & Dev Biol Program, Columbus, OH 43210 USA

[5] Shandong Univ, Sch Chem & Chem Engn, Jinan 250100, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2015年 / 23卷 / 06期

关键词：

STAT3; Inhibitor; SARs; SH2; Small organic molecule; Molecular docking; POTENT ANTITUMOR-ACTIVITY; SMALL-MOLECULE INHIBITOR; CANCER DRUG DISCOVERY; TRANSCRIPTIONAL CONTROL; ACTIVATION INHIBITOR; SIGNALING PATHWAY; INDUCE APOPTOSIS; MYELOMA CELLS; SH2; DOMAIN; IN-VIVO;

D O I：

10.1016/j.bmc.2015.01.025

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Inhibition of the signaling pathways of signal transducer and activator of transcription 3 (STAT 3) has shown to be a promising strategy to combat cancer. In this paper we report the design, synthesis and evaluation of a novel class of small molecule inhibitors, that is, XZH-5 and its analogues, as promising leads for further development of STAT3 inhibitors. Preliminary SARs was established for XZH-5 and its derivatives; and the binding modes were predicted by molecular docking. Lead compounds with IC50 as low as 6.5 mu M in breast cancer cell lines and 7.6 mu M in pancreatic cancer cell lines were identified. (C) 2015 Elsevier Ltd. All rights reserved.

引用

页码：1348 / 1355

页数：8

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