雌激素影響著人體生長發展、體內平衡與細胞再生，許多雌激素引發的效應都是透過與雌激素受體鍵結而發生的。近幾年雌激素衍生化產物廣為應用在研究與雌激素受體鍵結。
本論文使用雌酮為起始物以合成17α取代的雌二醇衍生物，在雌酮的羰基行加成反應後生成支鏈，接著將支鏈末端活化轉換成疊氮基，再還原後可得帶有胺基支鏈的雌激素衍生物。透過此合成步驟可提升產率並減短反應步驟而有效率的合成雌激素衍生物。
在雌激素受體鍵結分析的應用，利用標定Cy3的衍生物可偵測固定在晶片上的ER，將雌激素衍生物修飾在PDMS基材以製成小分子晶片，初步結果顯示所合成的雌激素衍生物可與雌激素受體產生鍵結，證明所合成之衍生物具有與受體鍵結的活性。

Estrogens are known to influence the growth, development, homeostasis, and reproductive system of the human body. Many effects of estrogens are mediated through its binding to the estrogen receptor (ER). In recent years, estrogen derivatives were synthesized to develop bioassays for ER bindings.
In this research, we used estrone as the starting material to synthesize 17α substituted estradiol. After adding a side chain to the carbonyl group of estrone, the terminus of the added side chain was activated and then converted to azide group, and then converted to amino group via reduction reaction. The total reaction yield was increased and the reaction time was greatly reduced compared to the reported method. Thus, the synthesis method developed in this study is efficient.
The synthesized estrogen derivatives were applied for receptor binding assays. The derivatives were labeled with Cy3 fluorescence dye and then applied to bind with the immobilized ER on PDMS chips. Small molecule chip was fabricated by immobilizing the synthesized estrogen derivatives on PDMS substrates. Preliminary results indicated that the synthesized estradiol derivatives conserved the binding affinity with ER.

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