Design and Synthesis of Pyridinylisoxazoles and Their Anticancer Activities

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 ) doi: 10.7503/cjcu20140333

Chemical Journal of Chinese Universities  2014, Vol. 35  Issue (12): 2584-2592    DOI: 10.7503/cjcu20140333

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:

Design and Synthesis of Pyridinylisoxazoles and Their Anticancer Activities YANG Hongliang1, XU Guoxing1, BAO Meiying2, ZHANG Dapeng1, LI Zhiwei1, PEI Yazhong1 1. The Center for Combinatorial Chemistry and Drug Discovery, School of Pharmaceutical Sciences, Jilin University, Changchun 130021, China; 2. Changchun Discovery Sciences Co. Ltd., Changchun 130012, China

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.

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http://www.cjcu.jlu.edu.cn/EN/10.7503/cjcu20140333     OR     http://www.cjcu.jlu.edu.cn/EN/Y2014/V35/I12/2584