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.
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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SF Yin, W Zhuang, WY Ma, ZG Wang, TD Wang, XH Chen , CN Zhang, . SYNTHESIS AND ANTITUMOR ACTIVITY OF 4-S-(5-AMIDO-1,3,4-THIODIAZOL-2-YL)4-DEOXY-4′-DEMETHYLEPIPODOPHYLLOTOXIN ANALOGUESJ. Acta Pharmaceutica Sinica, 1993, 28(10): 762-765.
Citation: SF Yin, W Zhuang, WY Ma, ZG Wang, TD Wang, XH Chen , CN Zhang, . SYNTHESIS AND ANTITUMOR ACTIVITY OF 4-S-(5-AMIDO-1,3,4-THIODIAZOL-2-YL)4-DEOXY-4′-DEMETHYLEPIPODOPHYLLOTOXIN ANALOGUESJ. Acta Pharmaceutica Sinica, 1993, 28(10): 762-765.
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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

SYNTHESIS AND ANTITUMOR ACTIVITY OF 4-S-(5-AMIDO-1,3,4-THIODIAZOL-2-YL)4-DEOXY-4′-DEMETHYLEPIPODOPHYLLOTOXIN ANALOGUES

    摘要
  • 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。

     

    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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