| 4-S-(5-酰氨基-1,3,4-噻二唑-2-基)-4-脱氧-4′-去甲基表鬼臼毒素衍生物的合成与抗肿瘤活性 |
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| 引用本文： | 尹述凡,庄武,马维勇,王志光,王天都,陈秀华,张椿年.4-S-(5-酰氨基-1,3,4-噻二唑-2-基)-4-脱氧-4′-去甲基表鬼臼毒素衍生物的合成与抗肿瘤活性[J].药学学报,1993,28(10):762-765. |
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| 作者姓名： | 尹述凡 庄武 马维勇 王志光 王天都 陈秀华 张椿年 |
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| 作者单位： | 上海医药工业研究院,上海200437 |
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| 摘 要： | 基于在4′-去甲基表鬼臼毒素母核C4位上联结含有杂原子的芳香环取代基,以此考察其结构与活性关系的设想,设计并合成了10个标题化合物。体外L1210白血病细胞与KB细胞生长抑制试验结果表明,这类化合物有较强的抗肿瘤活性。其中化合物SIPI-92-1772,1774,1775,1776,1777与1779的活性超过临床用药依托泊甙。其余化合物活性与依托泊甙相当或略低。
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| 关 键 词： | 鬼臼毒素 4-S-(5-酰氨基-1 3 4-噻二唑-2-基)-4-脱氧-4′-去甲基表鬼臼毒素衍生物 抗肿瘤活性 |
| 收稿时间： | 1992-11-18 |
SYNTHESIS AND ANTITUMOR ACTIVITY OF 4-S-(5-AMIDO-1,3,4-THIODIAZOL-2-YL)4-DEOXY-4′-DEMETHYLEPIPODOPHYLLOTOXIN ANALOGUES |
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| SF Yin,W Zhuang,WY Ma,ZG Wang,TD Wang,XH Chen and CN Zhang.SYNTHESIS AND ANTITUMOR ACTIVITY OF 4-S-(5-AMIDO-1,3,4-THIODIAZOL-2-YL)4-DEOXY-4′-DEMETHYLEPIPODOPHYLLOTOXIN ANALOGUES[J].Acta Pharmaceutica Sinica,1993,28(10):762-765. |
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| Authors: | SF Yin W Zhuang WY Ma ZG Wang TD Wang XH Chen and CN Zhang |
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| Abstract: | By the condensation of 4'-demethylepipodophyllotoxin with 2-amino-5-mereapto-1,3, 4-thiodiazole in CF3COOH and acylation in the presence of DEPC, 10 title compounds wereconveniently synthesized. These compounds were screened in vitro against L1210 leukemia and KB cells,in which compounds SIPI-92-1772, 1774, 1775, 1776, 1777 and 1779 exhibited more potent antitumor activity. |
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| Keywords: | 4-S-(5-Amido-1 3 4-thiodiazol-2-yl)4-deoxy-4′-demethylepi-podophyllotoxin analogues Antitumor activity Podophyllotoxin |
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