尹述凡, 马维勇, 王天都, 陈秀华, 张椿年. 4-(2-酰胺基-2-乙氧羰基)乙硫基-4-脱氧-4′-去甲表鬼臼毒素衍生物的合成与抗肿瘤活性J. 药学学报, 1993, 28(9): 668-672.
引用本文: 尹述凡, 马维勇, 王天都, 陈秀华, 张椿年. 4-(2-酰胺基-2-乙氧羰基)乙硫基-4-脱氧-4′-去甲表鬼臼毒素衍生物的合成与抗肿瘤活性J. 药学学报, 1993, 28(9): 668-672.
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SF Yin, WY Ma, TD Wang, XH Chen , CN Zhang, . SYNTHESIS AND ANTITUMOR ACTIVITY OF 4-(2-AMIDO-2-ETHOXYCARBONYL)ETHYLSULEENYL-4-DEOXY-4′-DEMETHYLEPIPODOPHYLLOTOXIN ANALOGUESJ. Acta Pharmaceutica Sinica, 1993, 28(9): 668-672.
Citation: SF Yin, WY Ma, TD Wang, XH Chen , CN Zhang, . SYNTHESIS AND ANTITUMOR ACTIVITY OF 4-(2-AMIDO-2-ETHOXYCARBONYL)ETHYLSULEENYL-4-DEOXY-4′-DEMETHYLEPIPODOPHYLLOTOXIN ANALOGUESJ. Acta Pharmaceutica Sinica, 1993, 28(9): 668-672.
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4-(2-酰胺基-2-乙氧羰基)乙硫基-4-脱氧-4′-去甲表鬼臼毒素衍生物的合成与抗肿瘤活性

SYNTHESIS AND ANTITUMOR ACTIVITY OF 4-(2-AMIDO-2-ETHOXYCARBONYL)ETHYLSULEENYL-4-DEOXY-4′-DEMETHYLEPIPODOPHYLLOTOXIN ANALOGUES

    摘要
  • 摘要: 为考察4′-去甲基表鬼臼毒素4位上取代基结构变化与抗肿瘤活性的关系,设计并合成了23个标题化合物。体外L1210白血病细胞与KB细胞生长抑制试验的结果表明,化合物11,16和18的抗肿瘤活性超过依托泊甙,化合物8的活性与依托泊甙相当。

     

    Abstract: Twenty three 4-(2-amido-2-ethoxycarbonyl) ethylsulfenyl-4-deoxy-4'-demethylepipodophyllotoxin analogues were synthesized by three steps, in which trifluoroacetic acid was used as a condensation agent of 4'-demethylepipodophyllotoxin with L-cysteine ethyl ester hydrochloride without any protection of phenolic hydroxy and amino groups. All compounds were screened in vitro against L1210 leukemia and KB cells, in which, compounds 11, 16 and 18 exhibited more potent antitumor activity than etoposide.

     

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