|YANG Hongliang, XU Guoxing, BAO Meiying, ZHANG Dapeng, LI Zhiwei, PEI Yazhong
Design and Synthesis of Pyridinylisoxazoles and Their Anticancer Activities
|2014 Vol. 35 (12): 2584-2592 [Abstract] ( 781 ) [HTML 0KB] [PDF 2464KB] (116 )
Abstract Based on the X-ray co-crystal structures of reported allosteric kinase inhibitors bound to their corresponding protein kinases, a pharmacophore model was proposed. To examine the validity of this hypothesis, 21 new pyridinylisoxazole derivatives were designed and synthesized. Their structures were confirmed using 1H NMR, 13C NMR and MS data. Their inhibitory effects against human breast cancer cell(MCF-7) proliferation were evaluated. Preliminary results indicated that some of these pyridinylisoxazole derivatives possess potent anti-proliferative activities, with IC50 data in the micromolar range. The mechanism-of-action of these compounds is under investigation.
|Cite this article:|
|YANG Hongliang,XU Guoxing,BAO Meiying et al. Design and Synthesis of Pyridinylisoxazoles and Their Anticancer Activities[J]. Chemical Journal of Chinese Universities, 2014, 35(12): 2584-2592.|
|http://www.cjcu.jlu.edu.cn/EN/10.7503/cjcu20140333 OR http://www.cjcu.jlu.edu.cn/EN/Y2014/V35/I12/2584|