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    Please use this identifier to cite or link to this item: http://ir.cmu.edu.tw/ir/handle/310903500/32616


    Title: Tetrahydroquinazolinone衍生物之合成與生物活性
    Synthesis and Biological Activities of Tetrahydroquinazolinone Derivatives
    Authors: 林品杉;Pin-Shan Lin
    Contributors: 藥學院藥物化學研究所碩士班
    Keywords: 四氫喹唑酮衍生物;抗軟骨細胞癌;抗發炎;tetrahydroquinazolines;anti-chondrosarcoma;anti-inflammatory
    Date: 2010
    Issue Date: 2010-09-29 14:10:26 (UTC+8)
    Abstract: 本論文將兩種具有抗癌活性結構1,8-naphthyridinones和aminopyrimidines融合，設計新穎的tetrahydroquinazolines (TQ) 構型，並探討此類化合物的SAR (structure-activity relationships)。初步結果顯示TQ第二位氮原子的取代以3-chlorophenyl及4-chlorophenyl取代具有較佳的抗軟骨細胞活性 (chondrosarcoma, JJ)，若將TQ結構的第五位置carbonyl基團，置換成hydroxyamine取代時則能增加抗骨癌活性。抗發炎方面主要在探討TQ結構對於N-formyl-methionyl-leucylphenylalanine (fMLP) 在人類嗜中性白血球所引起的超氧自由基生成表現的影響，其中，以2-chlorophenyl與2-fluorophenyl為具有最佳作用的活性成分。相同的，若將TQ結構的第五位置carbonyl基團，置換成hydroxyamine取代時則能增加抗發炎活性。

    This research is about the integration of two anti-tumor structures, which are 1,8-naphthyridinones and aminopyrimidines, designing novel tetrahydroquinazolines (TQ) derivatives and confering a series of TQ derivatives. Preliminary results showed that the introduction of 3-chlorophenyl and 4-chlorophenyl into 2-position of amino group on TQ increased the activity against chondrosarcoma (JJ). Moreover, the replacement of 5-carbonyl group with hydroxyamine group dramatically enhanced the anti-chondrosarcoma activity. To the anti-inflammatory study, we focus on the structure-activity relationship of TQ for the effect of N-formyl-methionyl-leucylphenylalanine (fMLP) in human neutrophils induced by superoxide anion (O2•−) generation in human neutrophils. Preliminary results showed that the introduction of 2-chlorophenyl and 2-fluorophenyl into 2-position of amino group on TQ increased the activity against inflammatory. The same, replace the 5 - carbonyl and hydroxyamine group significantly increased the activities of the anti-inflammatory.
    Appears in Collections:[Graduate Institute of Pharmaceutical Chemistry] Theses & dissertations

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