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为了考察鬼臼毒素 C_4位侧链取代基变化对活性的影响,合成28个标题化合物。体外 L1210白血病细胞及 KB 细胞生长抑制试验结果,表明所有化合物均具不同程度的抗肿瘤活性,其中化合物(1)、(5)和(8)～(10)的活性超过临床用药依托泊甙。
In order to investigate the effect of the change of substituents on the side chain of C_4 position of podophyllotoxin, 28 title compounds were synthesized. In vitro L1210 leukemia cells and KB cell growth inhibition test results show that all compounds have varying degrees of anti-tumor activity, of which compounds (1), (5) and (8) ~ (10) activity over the clinical use of etoposide.