English  |  正體中文  |  简体中文  |  全文筆數/總筆數 : 18034/20233 (89%)
造訪人次 : 23348427      線上人數 : 496
RC Version 7.0 © Powered By DSPACE, MIT. Enhanced by NTU Library IR team.
搜尋範圍 查詢小技巧:
  • 您可在西文檢索詞彙前後加上"雙引號",以獲取較精準的檢索結果
  • 若欲以作者姓名搜尋,建議至進階搜尋限定作者欄位,可獲得較完整資料
  • 進階搜尋
    請使用永久網址來引用或連結此文件: https://ir.cnu.edu.tw/handle/310902800/24208


    標題: Synthesis and Biological Evaluation of Small Molecular Compounds as Potent Antimitotic/Vascular Disrupting Agents
    作者: Jing-Ping Liou (劉景平)
    日期: 2011
    上傳時間: 2011-06-23 14:57:02 (UTC+8)
    摘要: A series of aroylquinoline derivatives ([6,6]-fused heterocycle) were synthesized and evaluated for anticancer activity. 5-Amino-6-methoxy-2-aroylquinoline 15 showed more potent antiproliferative activity (IC50 values ranging from 0.2 to 0.4 nM) as compared to combretastatin A-4 (CA4, IC50 = 1.9-835 nM) against various human cancer cell lines and a MDR-resistant cancer cell line. Compound 15 (IC50 = 1.6 μM) exhibited more potent inhibition of tubulin polymerization than CA4 (IC50 - 2.1 μM) and showed strong binding property to the colchicine binding site of microtubules. In an attempt to mimic the 3,4,5-trimethoxyphenyl-Z-stilbene moiety of combretastatin A-4, a series of N-aryl-5,6,7-trimethoxyindoldes ([6,5]-fused tieterocycle) were synthesized via copper-catalyzed Ullmann-tyfype N-aryarylation through corresponding 5,6,7-trimethoxyindole and aryl halides. These synthesized compounds demonstrated potent antiproliferative activity providing a novel skeleton for potent tubulin polymerization inhibitors. Compound 6 demonstrated substantial vascular disrupting activity (VDA), which was capable to disrupt formed capillaries in concacentration-dependent manner without affecting cell viability.
    關聯: 2011年台俄有機、藥物與生物化學交流暨藥物化學研討會,起迄日:2011/04/06~2011/04/05,地點:溪頭台大實驗林
    顯示於類別:[藥理學院] 2011年台俄有機、藥物與生物化學交流暨藥物化學研討會

    文件中的檔案:

    檔案 描述 大小格式瀏覽次數
    il-08.pdf78KbAdobe PDF400檢視/開啟


    在CNU IR中所有的資料項目都受到原著作權保護.

    TAIR相關文章

    DSpace Software Copyright © 2002-2004  MIT &  Hewlett-Packard  /   Enhanced by   NTU Library IR team Copyright ©   - 回饋