王志光, 尹述凡, 马维勇, 李炳生, 张椿年. 4-酰胺基-4-脱氧-4′-去甲表鬼臼毒素衍生物的合成和抗肿瘤活性J. 药学学报, 1993, 28(6): 422-427.
引用本文: 王志光, 尹述凡, 马维勇, 李炳生, 张椿年. 4-酰胺基-4-脱氧-4′-去甲表鬼臼毒素衍生物的合成和抗肿瘤活性J. 药学学报, 1993, 28(6): 422-427.
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ZG Wang, SF Yin, WY Ma, BS Li , CN Zhang, . SYNTHESIS AND ANTITUMOR ACTIVITIES OF 4-ACYLAMIDO-4-DEOXY-4′-DEMETHYLEPIPODOPHYLLOTOXIN ANALOGUESJ. Acta Pharmaceutica Sinica, 1993, 28(6): 422-427.
Citation: ZG Wang, SF Yin, WY Ma, BS Li , CN Zhang, . SYNTHESIS AND ANTITUMOR ACTIVITIES OF 4-ACYLAMIDO-4-DEOXY-4′-DEMETHYLEPIPODOPHYLLOTOXIN ANALOGUESJ. Acta Pharmaceutica Sinica, 1993, 28(6): 422-427.
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4-酰胺基-4-脱氧-4′-去甲表鬼臼毒素衍生物的合成和抗肿瘤活性

SYNTHESIS AND ANTITUMOR ACTIVITIES OF 4-ACYLAMIDO-4-DEOXY-4′-DEMETHYLEPIPODOPHYLLOTOXIN ANALOGUES

    摘要
  • 摘要: 4′-去甲表鬼臼毒素与叠氮酸在三氟化硼乙醚存在下缩合,并经还原得4-氨基-4-脱氧-4′-去甲表鬼臼毒素。该中间体与酸或酸酐反应得相应酰胺化合物24个。经体外筛选,多数化合物抑制L1210和KB细胞活性相当或超过依托泊甙。与相应的醚、酯、胺等类型相比,这一类化合物活性最强。

     

    Abstract: Twenty four 4-acylamidc-4-deoxy-4'-demethylepipodophyllotoxins were synthesized by acylation of 4-amino-4-deoxy-4'-demethylepipodophyllotoxin by means of usual methods, and screened in vitro. This type of compounds showed strong antitumor activities, most of them are superior to etoposide in the inhibition against L1210 and KB cells.

     

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