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

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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:	[Graduate Institute & Department of Chemistry] Thesis

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