| DC 欄位 |
值 |
語言 |
| DC.contributor | 化學學系 | zh_TW |
| DC.creator | 呂柏葦 | zh_TW |
| DC.creator | Po-wei Lu | en_US |
| dc.date.accessioned | 2013-8-26T07:39:07Z | |
| dc.date.available | 2013-8-26T07:39:07Z | |
| dc.date.issued | 2013 | |
| dc.identifier.uri | http://ir.lib.ncu.edu.tw:88/thesis/view_etd.asp?URN=100223042 | |
| dc.contributor.department | 化學學系 | zh_TW |
| DC.description | 國立中央大學 | zh_TW |
| DC.description | National Central University | en_US |
| dc.description.abstract | 近年來，癌症的轉移往往伴隨唾液酸轉移酶的異常表現，因此發展唾液酸轉
移酶的抑制劑，並測試其抑制活性，了解化合物結構與抑制能力的關係，期望能
以抑制唾液酸轉移酶為分子標靶來達到抗癌症轉移的效果。
以Lith-O-Asp 為主結構，並透過DMMTM BF4 耦合試劑和SOCl2 醯氯化合
成醯胺鍵連接一系列的香豆素衍生物，分別透過細胞傷口癒合分析及唾液酸轉移
酶抑制實驗來探討香豆素衍生物上的取代基對於生物活性的影響。透過生物實驗
可以發現KE-49、KE-50、KE-89 及KE-126 有較明顯的抑制能力，代表香豆素
上的羥基有助於增進抑制活性，其中又以C7 號位的羥基取代最為明顯，另外在
C8 號位增加一個甲基取代也有助於活性的提升。 | zh_TW |
| dc.description.abstract | Recently, aberrant sialylation is found in cancer metastasis frequently.
Empolying the strategy of the relationships between structure and activity , we use
sialyltrasdferase as the molecular target to develop its inhibitors in order to attenuate
cancer metastasis.
Preparation of Lith-O-Asp-coumarin derivatives was successfully accomplished
through the coupling reaction between Lith-O-Asp and coumarin moieties using
DMMTM BF4 (4-(4,6-dimethoxy-(1,3,5)triazin-2-yl)-4-methyl-morpholinium tetrafluoroborate)
or SOCl2 as the reagents. Extensive SAR studies were performed using
different substituted-coumarin analogs under the wound healing and sialyltransferase
inhibitor assays. Among the Lith-O-Asp-coumarin derivatives, the
hydroxyl-substituent analogs at C-7 position were observed to have the hightest
biological activity. It is also noteworthy that the methyl-substituent analogs at C-8
position also display significantly increased biological activity toward both assays. | en_US |
| DC.subject | 唾液酸 | zh_TW |
| DC.subject | 唾液酸轉移酶 | zh_TW |
| DC.subject | 香豆素 | zh_TW |
| DC.subject | sialic acid | en_US |
| DC.subject | Sialyltransferase | en_US |
| DC.subject | Coumarin | en_US |
| DC.title | 含有香豆素的石膽酸類似物作為唾液酸轉移酶抑制劑的合成與初步活性測試 | zh_TW |
| dc.language.iso | zh-TW | zh-TW |
| DC.title | A Series of Lithocholic Acid Analogs with Coumarin Moieties as Sialyltransferase Inhibitors: Synthesis and Preliminary Bioactivity Studies | en_US |
| DC.type | 博碩士論文 | zh_TW |
| DC.type | thesis | en_US |
| DC.publisher | National Central University | en_US |