Design, synthesis and evaluation of quinoline-based small molecule inhibitor of STAT3

…, L Zhang, ZY Bin, XR Cao, ZN Gong…

文献索引：Shi, Zhi-Bing; Zhang, Lei; Bin, Zheng-Yang; Cao, Xiang-Rong; Gong, Zhu-Nan; Li, Jian-Xin Letters in Drug Design and Discovery, 2013 , vol. 10, # 5 p. 420 - 426

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被引用次数: 2

摘要

As STAT3 has been validated as an anticancer target, its inhibitors have been shown to possess therapeutic promise for the treatment of human cancers. To identify novel and selective STAT3 inhibitors, a virtual screening based on the STAT3 SH2 domain was performed and a small molecule, 2-phenylquinoline-4-carboxylic acid (5a), with an inhibition constant Ki value of 17.53 μM to STAT3 was discovered. On this basis, the derivatives of ...