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为考察 4′ 去甲鬼臼毒素C4位上联结碳原子对活性的影响 ,作者设计并合成C4位 β构型的硫酯取代的衍生物 18个 .这类化合物在体外的抑制L12 10细胞和KB细胞的药理实验中显示出一定的抗肿瘤活性 ,但均弱于etoposide
In order to investigate the effect of 4 carbon atoms on the C4 position of depolazinotoxin 4, the authors designed and synthesized thioester-substituted derivatives of C4-position β-configuration, and these compounds inhibit the activity of L12 10 cells and Pharmacological experiments of KB cells showed some anti-tumor activity, but both were weaker than etoposide