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4’-去甲表鬼臼毒素与巯基乙胺在三氟乙酸存在下反应,再经 N-酰化或还原胺化得相应的衍生物共20个。体外药理筛选结果显示这些化合物对 L 1210有抑制活性,但活性比依托泊甙差;对 KB 细胞仅在高浓度显示活性。
4’-norvodipodophyllotoxin and mercaptoethylamine in the presence of trifluoroacetic acid, followed by N-acylation or reductive amination to give a total of 20 corresponding derivatives. In vitro pharmacological screening showed that these compounds have inhibitory activity against L1210 but less activity than etoposide; KB cells show activity only at high concentrations.