表鬼臼毒素羧酸酯的合成及体外抗肿瘤活性
SYNTHESIS OF EPIPODOPHYLLOTOXIN CARBOXYLATES AND ANTITUMOR ACTIVITY IN VITRO
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摘要: 在三氟化硼·乙醚的催化作用下,鬼臼毒素(I)与有机酸直接脱水生成了具有4β-构型的表鬼臼毒素羧酸酯(IIa~g),所有合成产物经IR,1HNMR,MS和元素分析等确证其结构,初步药理试验表明,该类化合物对小鼠白血病P388、人胃癌SGC-7901有一定的抑制活性。Abstract: A series of epipodophyllotoxin carboxylates were prepared from podophyllotoxin by reacting with organic acids under the catalysis of BF3·Et2O. All these products were characterized through IR, 1HNMR, MS and elemental analysis.These compounds showed significant antitumor activities against mouse leukemia P388 and human stomach cancer SGC-7901 in pharmacological tests in vitro.
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