Antagonizing STAT3 activation with benzo[b]thiophene 1, 1-dioxide based small molecules

详细信息    查看全文

• 作者：Wenda Zhang ; Ting Ma ; Shanshan Li ; Yanwei Yang ; Jianpeng Guo ; Wenying Yu ; ^{ywy@cpu.edu.cn} ; Lingyi Kong ; ^{cpu_lykong@126.com}
• 关键词：Antitumor agents ; Aminobenzo[b]thiophene 1 ; 1-dioxides ; Drug-likeness properties ; STAT3 phosphorylation ; Apoptosis
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：5 January 2017
• 年：2017
• 卷：125
• 期：Complete
• 页码：538-550
• 全文大小：2609 K
• 卷排序：125

文摘

24 new BTP derivatives were developed as STAT3 inhibitors for anticancer agents. 15 exhibited potent antitumor activity in vitro and in vivo. 15 selectively inhibited STAT3 activity without affecting the upstream kinases. 15 exhibited less toxicity than Doxorubicin in vivo. Docking study was conducted to further understand the SAR.