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    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
    含硼之胜肽衍生物合成與其生物活性評估
    利用Passerini反應合成含硼之衍生物
    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:
    本論文中我們設計與合成了兩系列含硼胜肽化合物。此類化合物可以以簡單的合成方法製備與純化。同時也使用了HepG2(肝癌)和MDA-MB231(乳癌)兩種癌細胞,來評估所合成之化合物的抗癌能力。藉由改變含硼化合物之結構來探討分子結構與生物活性之關係。
    第二部分:
    近年來由於含硼化合物在藥物開發上逐漸受到注意,因此含硼化合物的合成也逐漸受到重視。本研究利用Passerini三單元組成反應成功的合成出一系列的含硼化合物。由於多單元組成反應具備操作簡單、產物產出快速等優點,因此非常適合應用於含硼藥物的開發上。
    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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