Design, synthesis and evaluation of quinoline-based small molecule inhibitor of STAT3
…, L Zhang, ZY Bin, XR Cao, ZN Gong…
Index: 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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Abstract
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 ...
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