國家衛生研究院 NHRI:Item 3990099045/6815
English  |  正體中文  |  简体中文  |  全文筆數/總筆數 : 12145/12927 (94%)
造訪人次 : 913662      線上人數 : 1193
RC Version 6.0 © 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
    主頁 ‧ 登入 ‧ 上傳 ‧ 說明 ‧ 關於NHRI ‧ 管理 到手機版


    請使用永久網址來引用或連結此文件: http://ir.nhri.org.tw/handle/3990099045/6815


    題名: Concise synthesis and structure-activity relationships of combretastatin A-4 analogues, 1-aroylindoles and 3-aroylindoles, as novel classes of potent antitubulin agents
    作者: Hsieh, HP;Liou, JP;Chang, YL;Lee, SJ
    貢獻者: Institute of Biotechnology and Pharmaceutical Research
    摘要: The synthesis and study of structure-activity relationship of two new classes of synthetic antitubulin compounds based on 1-aroylindole and 3-aroylindole skeleton are described. Lead compounds 3, 10 and 14 displayed potent cytotoxicity with IC50 = 0.9 to 22 nM against human NUGC3 stomach, MKN45 stomach, MESSA uterine, A549 lung, and MCF-7 breast carcinoma cell lines. The inhibition of proliferation correlated with in vitro polymerization inhibitory activities. Structure-activity relationships revealed that 6-methoxy substitution of 3-aroylindoles and 5-methoxy substitution of 1-aroylindoles contributes to a significant extent for maximal activity by mimicking the para substitution of the methoxy group to the carbonyl group in case of aminobenzophenones. Addition of a methyl group at the C-2 position on indole ring exerts increased potency. 3,4,5-Trimethoxybenzoyl moiety was necessary for better activity, but not essential and can be replaced by 3,5-dimethoxybenzoyl and 3,4,5-trimethoxybenzyl moieties. We conclude that 1- and 3-aroylindoles constitute an interesting new class of antitubulin agents with the potential to be clinically developed for cancer treatment.
    日期: 2004-08-22
    關聯: Abstracts of Papers - American Chemical Society. 2004 Aug 22;228:U924.
    Link to: http://oasys2.confex.com/acs/228nm/techprogram/P756903.HTM
    Cited Times(WOS): https://www.webofscience.com/wos/woscc/full-record/WOS:000223712803928
    顯示於類別:[謝興邦] 會議論文/會議摘要
    [李秀珠] 會議論文/會議摘要

    文件中的檔案:

    沒有與此文件相關的檔案.



    在NHRI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