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    題名: Synthesis of 2-styrylchromones as a novel class of antiproliferative agents targeting carcinoma cells
    作者: 蕭永政;Shaw, Arthur Y.;Chang, Chun-yi;Liau, Hao-han;Lu, Pei-jung;Chen, Hui-ling;Yang, Chia-ning;Li, Hao-yi
    貢獻者: 淡江大學化學學系
    日期: 2009-06
    上傳時間: 2010-08-09 15:51:33 (UTC+8)
    出版者: Elsevier
    摘要: A series of 2-styrylchromone analogs were synthesized and examined for their antiproliferative effects on a panel of carcinoma cells. Among the tested agents, only 4m exhibited a moderate activity with an IC50 value of 28.9 μM against PC-3 cells which indicates the selectivity of PC-3 cells in response to 2-styrylchromones. In addition, 4q demonstrated the most antiproliferative effect with an IC50 value of 4.9 μM against HeLa cells. Flow cytometric analysis and DAPI staining revealed that HeLa cells exposed to 4q as low as 5 μM induced cell death through sub-G1 arrest and DNA fragmentation. Furthermore, CoMFA analysis of tested 2-styrylchromones resulted in a q2 of 0.459 to generate a 3D-QSAR model on BT483 cell line. Together, these results suggest a potential structural optimization and pharmacological study of 2-styrylchromones.
    關聯: European Journal of Medicinal Chemistry 44(6), pp.2552-2562
    DOI: 10.1016/j.ejmech.2009.01.034
    顯示於類別:[化學學系暨研究所] 期刊論文


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