查詢結果分析
相關文獻
- Preparation and Antitumor Activities of β-Azatyrosinamides
- 自乳清蛋白水解液中製備血管收縮素轉化酶抑制劑之研究
- 九節木之活血化瘀活性分析
- Mechanism of Action Based Design and Development of Newer Synthetic Antitumor Agents
- 自明膠水解液中製備血管收縮素轉化酶抑制劑之研究
- Lactobacillus Reuteri甘油代謝物對微生物與癌細胞株抑制性之探討
- 設計及合成8-胺基比咯苯偶氮駢混成抗癌試劑
- 樟芝固體栽培及其生物活性之研究
- Pharmacological Functions of Chinese Medicinal Fungus Cordyceps sinensis and Related Species
- 中藥及臺灣產天然物抗病毒抗癌及抗血栓之研究
頁籤選單縮合
題 名 | Preparation and Antitumor Activities of β-Azatyrosinamides=β-Azatyrosinamides之合成及抗癌活性研究 |
---|---|
作 者 | 王惠珀; 吳銘芳; 李昂; 許金玉; 李淑娟; 宋啟華; | 書刊名 | 藥物食品分析 |
卷 期 | 8:3 2000.09[民89.09] |
頁 次 | 頁159-165 |
分類號 | 418.27 |
關鍵詞 | 抗癌活性; IC叙; Azatyrosine; PC-3 prostate cancer cell line; Ras-transformed NIH3T3 cell lie; |
語 文 | 英文(English) |
英文摘要 | A large number of human prostate cancer cases has been proven to be genetically associated with ras-mutation. A series of a-azatyrosinamides prepared in this laboratory demonstrated selective cytotoxicity against ras-mutated NIH3T3 cells while with little toxicity on wild type NIH3T3 cells. The compounds also proved to be active in inhibiting human prostate cancer cell lines. Using a-azatyrosinamides as the leads, we prepared another series of novel b-azatyrosinamides for the purpose of treating human prostate cancer. Preparation of the b-azatyrosinamides starts from 5- benzyloxypyridin-2-ylaldehyde (1), which upon reaction with malonic acid and ammonium acetate afforded 5-benzyloxy-b-azatyrosine (2). This intermediate was allowed to react with benzyloxycarbonic anhydride followed by coupling with a variety of amines to form the desired b-azatyrosinamides 4-15. The compounds exhibited an inhibitory effect on the growth of ras-mutated NIH3T3 cells with IC50 ranged between 0.13±0.01 mM and 3.16±1.45 mM, which were with activities 2-57 fold higher than that of azatyrosine, but were much less active than their a-amino acid analogues. The selective toxicity, in terms of the ratio of IC50 against wild type NIH3T3 to that against ras-transformed NIH3T3 cell lines, is at the range of 0.7-11.9. The IC50's of b-azatyrosinamides 4-15 on PC-3 human prostate cancer cell line ranged between 0.15±0.02 mM and 13.05±9.41 mM, which were 0.4-33 fold lower than that of azatyrosine. |
本系統中英文摘要資訊取自各篇刊載內容。