中國醫藥大學機構典藏 China Medical University Repository, Taiwan:Item 310903500/46315
English  |  正體中文  |  简体中文  |  Items with full text/Total items : 29490/55136 (53%)
Visitors : 1997707      Online Users : 114
RC Version 7.0 © Powered By DSPACE, MIT. Enhanced by NTU Library IR team.
Scope Tips:
  • please add "double quotation mark" for query phrases to get precise results
  • please goto advance search for comprehansive author search
    •  Adv. Search
    Home ‧ Login ‧ Upload ‧ Help ‧ About ‧ Administer Goto mobile version


    Please use this identifier to cite or link to this item: http://ir.cmu.edu.tw/ir/handle/310903500/46315


    Title: 化學選擇性合成1H-pyrazol-5-yl-N,N-dimethylformamidines和pyrazolyl-2-azadienes新方法暨抗癌活性之探討
    Chemoselective synthesis, antiproliferative activities and SAR study of 1H-pyrazol-5-yl-N,N-dimethylformamidines and pyrazolyl-2-azadienes
    Authors: 温國山;Wen, Kuo-Shan
    Contributors: 藥物化學研究所碩士班
    Keywords: 吡唑;微波加速反應;醋酸甲脒;Pyrazoles;Microwave-assisted reaction;Methnimidamide
    Date: 2012-06-15
    Issue Date: 2012-09-03 10:00:24 (UTC+8)
    Publisher: 中國醫藥大學
    Abstract: 本論文是利用微波加速化學反應及化學選擇性控制方法，合成出1H-pyrazol-5-yl-N,N-dimethyl-formamidine和pyrazolyl-2-azadiene的兩類化合物，將5-amino-1,3-diphenyl pyrazole，1H-pyrazol-5-yl-N,N-dimethyl-formamidines，pyrazolyl-2-azadiene，5-amino-4-formylpyrazoles四類具構效關係的化合物經由藥理活性篩選 (NCI-H661，NPC-TW01，Jurkat)。

    其結果顯示1H-pyrazol-5-yl-N,N-dimethylformamidines衍生物2b，2c，2d具較佳的藥理活性 (IC50: 6.0~9.2μM)，從藥理活性也指出在pyrazole derivatives須同時擁有amidinyl與formyl官能基才能增強藥理活性。

    Chemoselective microwave-assisted amidination was successfully developed to alternatively synthesize 1H-pyrazol-5-yl-N,N-dimethyl-formamidine and pyrazolyl-2-azadiene two classes compounds. All of the starting materials and resulting products were tested against NCI-H226, NPC-TW01, and Jurkat cancer cell lines to evaluate their difference in antiproliferative activities for realizing the structure activity relationship study.
    Following the SAR result, 1H-pyrazol-5-yl-N,N-dimethylformamidine compounds 2b, 2c and 2d possessed the best potent with IC50 values in low micromolar range. On the other hand, we found that the formyl group at C-4 position and the grafted amidinyl group in the main core of pyrazolic molecule were necessary for the inhibitory activity.
    Appears in Collections:[Graduate Institute of Pharmaceutical Chemistry] Theses & dissertations

    Files in This Item:

    File Description SizeFormat
    cmu-101-9963008-1.pdf3417KbAdobe PDF353View/Open
    index.html0KbHTML9View/Open


    All items in CMUR are protected by copyright, with all rights reserved.

     

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