3α-溴-表苦鬼臼脂素及其衍生物:具抗癌活性的鬼臼脂素新类似物

3α-溴-表苦鬼臼脂素及其衍生物:具抗癌活性的鬼臼脂素新类似物

何勇, 马维勇, 张椿年

上海医药工业研究院, 上海 200040

收稿日期:2001-02-15 修回日期:2001-03-12 出版日期:2001-06-15 发布日期:2001-06-15

3α-Bromo-epipicropodophyllin and Its Derivatives: Novel Analogues of Podophyllotoxin with Antitumor Activities

He Yong, Ma Weiyong, Zhang Chunnian

Shanghai Institute of Pharmaceutical Industry, 1320 Beijing Xi Road, Shanghai 200040

Received:2001-02-15 Revised:2001-03-12 Online:2001-06-15 Published:2001-06-15

摘要/Abstract

摘要： 本文制备了3α-溴-表苦鬼臼脂素,首次在鬼臼脂素结构修饰中在C环3-位引入取代基。其体外抑制KB细胞和L1210白血病细胞活性均高于阳性对照药。在碱性条件下,其可被方便地转化为4β-羟基-2,3-不饱和苦鬼臼脂素,进而2,3-不饱和鬼臼脂素衍生物可被合成。由于具有较好的体外抑制肿瘤细胞活性,该化合物可作为结构修饰的先导化合物。由于3-位溴原子的引入,其又是鬼臼脂素类化合物结构转化的中间体。

关键词: 鬼臼脂素, 鬼臼脂素类似物, 抗肿瘤活性

Abstract: 3α-bromo-epipicropodophyllin was prepared and its inhibition activities against KB cells and L1210 leukemia cells in vitro are higher than those of VP-16, a widely used drug in clinic at present. This is the first time to introduce substitution at C-3 of ring-C in the work of modifying structure of podophyllotoxin. It can be transformed easily to 4β-hydroxy-2,3-ene-apopicropodophyllin under basic condition, so that, corresponding derivatives of 2,3-ene-apopicropodophyllin with substitution on carbon-4 could be synthesized. This compound can be regarded not only as a leading compound to be modified because of its antitumor activities, but also as an intermediate for the structure transformation.

Key words: Podophyllotoxin, Podopgyllotoxin analogues, Antitumor activities

Supporting:

何勇, 马维勇, 张椿年. 3α-溴-表苦鬼臼脂素及其衍生物:具抗癌活性的鬼臼脂素新类似物[J]. .

He Yong, Ma Weiyong, Zhang Chunnian . 3α-Bromo-epipicropodophyllin and Its Derivatives: Novel Analogues of Podophyllotoxin with Antitumor Activities[J]. .

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