| 4-酰胺基-4-脱氧-4′-去甲表鬼臼毒素衍生物的合成和抗肿瘤活性 |
| |
| 引用本文： | 王志光,尹述凡,马维勇,李炳生,张椿年. 4-酰胺基-4-脱氧-4′-去甲表鬼臼毒素衍生物的合成和抗肿瘤活性[J]. 药学学报, 1993, 28(6): 422-427 |
| |
| 作者姓名： | 王志光 尹述凡 马维勇 李炳生 张椿年 |
| |
| 作者单位： | 上海医药工业研究院,上海200437 |
| |
| 摘 要： | 4′-去甲表鬼臼毒素与叠氮酸在三氟化硼乙醚存在下缩合,并经还原得4-氨基-4-脱氧-4′-去甲表鬼臼毒素。该中间体与酸或酸酐反应得相应酰胺化合物24个。经体外筛选,多数化合物抑制L1210和KB细胞活性相当或超过依托泊甙。与相应的醚、酯、胺等类型相比,这一类化合物活性最强。
|
| 关 键 词： | 鬼臼毒素衍生物 抗肿瘤活性 |
| 收稿时间： | 1992-07-29 |
SYNTHESIS AND ANTITUMOR ACTIVITIES OF 4-ACYLAMIDO-4-DEOXY-4′-DEMETHYLEPIPODOPHYLLOTOXIN ANALOGUES |
| |
| ZG Wang,SF Yin,WY Ma,BS Li and CN Zhang. SYNTHESIS AND ANTITUMOR ACTIVITIES OF 4-ACYLAMIDO-4-DEOXY-4′-DEMETHYLEPIPODOPHYLLOTOXIN ANALOGUES[J]. Acta pharmaceutica Sinica, 1993, 28(6): 422-427 |
| |
| Authors: | ZG Wang SF Yin WY Ma BS Li CN Zhang |
| |
| Abstract: | Twenty four 4-acylamidc-4-deoxy-4'-demethylepipodophyllotoxins were synthesized by acylation of 4-amino-4-deoxy-4'-demethylepipodophyllotoxin by means of usual methods, and screened in vitro. This type of compounds showed strong antitumor activities, most of them are superior to etoposide in the inhibition against L1210 and KB cells. |
| |
| Keywords: | 4-Acylamido- 4-deoxy- 4'-demethylepipodophyllotoxin Antitumor activity Podophyllotoxin derivatives |
| 本文献已被 维普 等数据库收录！ |
| 点击此处可从《药学学报》浏览原始摘要信息 |
|
点击此处可从《药学学报》下载全文 |
|
