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    Please use this identifier to cite or link to this item: http://tkuir.lib.tku.edu.tw:8080/dspace/handle/987654321/87428

    Title: 第一部分 : 含硼之胜肽衍生物合成與其生物活性評估;第二部分 : 利用Passerini反應合成含硼之衍生物
    Other Titles: (I) synthesis and biological evaluation of boron-containing peptide : based analogues;(II) synthesis of passerini-type boron-containing analogues
    Synthesis and biological evaluation of boron-containing peptide : based analogues
    Synthesis of passerini-type boron-containing analogues
    Authors: 林家弘;Lin, Chia-Hung
    Contributors: 淡江大學化學學系碩士班
    潘伯申;Pan, Po-Shen
    Keywords: 含硼胜肽化合物;passerini多組成反應;boron-containing peptide analogues;passerini multicompoent reaction
    Date: 2012
    Issue Date: 2013-04-13 11:04:42 (UTC+8)
    Abstract: 第一部分:
    part 1
    In this project, we have designed and synthesized two series of boron-containing analogues. These analogueswere synthesized via facile and efficientsynthetic operations.
    The anticancer potency of the synthesized boron-containing derivatives were evaluated by two cancer cell lines: HepG2 (liver cancer) and MDA-MB231 (drug resistant breast cancer). The structure-activity relationship (SAR) profiles indicated that inclusions of aphenylalanine in position 2, benzyl-protected serine in position 3, and a potassium trifluoroborate functional group greatly improved the compound’s ability against HepG2 and MDA-MB231 cell lines.

    part 2
    In recent years, boron-containing compounds havedrawn the attention of medicinal research communityafter the success of the FDA approved drug: Velcade. In the second project, we have utilized the Passerini-type 3components reaction (P3CR) to construct series of boron-containing derivatives. Although the reaction condition was not yet optimized, the result have shown the novel protocol of generating structurally diverse boron-containing analogues via multicomponent reaction.
    Appears in Collections:[化學學系暨研究所] 學位論文

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