| 三尖杉碱酯类化合物的合成及其抗肿瘤活性 |
| |
| 引用本文： | 李述文,孙菡丽,卢秀静,张素胤,吕腓理,戴金嫒,徐仪宝.三尖杉碱酯类化合物的合成及其抗肿瘤活性[J].药学学报,1981,16(11):821-827. |
| |
| 作者姓名： | 李述文 孙菡丽 卢秀静 张素胤 吕腓理 戴金嫒 徐仪宝 |
| |
| 作者单位： | 中国科学院上海药物研究所，中国科学院上海药物研究所，浙江人民卫生实验院药物研究所，中国科学院上海药物研究所，中国科学院上海药物研究所，中国科学院上海药物研究所，中国科学院上海药物研究所 上海，上海，上海，上海，上海，上海 |
| |
| 摘 要： | 脱氧三尖杉酯碱Ⅰ。对动物肿瘤P-388有明显的抑制作用。本文报道了三尖杉碱的十二个新的酯类化合物的合成及其抗肿瘤作用。药理实验发现合成的脱氧三尖杉酯碱(差向异构物混合体)有一定的抗肿瘤作用。通过化学结构和抗肿瘤活性的比较,初步推断酯碱Ⅰ.侧链的异丙基和α-叔羟基及甲氧羰甲基是抗肿瘤所必需的结构。
|
| 收稿时间： | 1980-08-06 |
SYNTHESIS OF CEPHALOTAXINE ESTERS AND THEIR ANTITUMOR ACTIVITY |
| |
| SYNTHESIS OF CEPHALOTAXINE ESTERS AND THEIR ANTITUMOR ACTIVITY.SYNTHESIS OF CEPHALOTAXINE ESTERS AND THEIR ANTITUMOR ACTIVITY[J].Acta Pharmaceutica Sinica,1981,16(11):821-827. |
| |
| Authors: | SYNTHESIS OF CEPHALOTAXINE ESTERS AND THEIR ANTITUMOR ACTIVITY |
| |
| Abstract: | Harringtonine (Ⅰa), homoharringtonine (Ⅰb), and deoxyharringtonine (Ⅰc) isolated from Cephalotaxus plant material are known as the esters of cephalotaxine with significant inhibitory activity against P-388 leukemia. In this investigation twelve new esters of natural cephalotaxine have been synthesized. The preparation of cephalotaxine esters was carried out by direct acylation. Preliminary pharmacological examination showed that synthetic deoxyharringtonine (Ⅰc) and compound (Ⅰe) exhibited significant inhibitory action on leukemia 615 and brain tumor 22 in mice. An interesting feature observed in these structure activity correlation is that the isopropyl, the tertiaty hydroxyl group and the methoxycarbonymethyl group are essential moiety of their side chain for tumor inhibition. |
| |
| Keywords: | |
| 本文献已被 CNKI 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》下载免费的PDF全文 |
