摘要
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。
The synthesis and antitumor activities of 4-(2-aminoethylthio)4-deoxy-4′-demethylepipodophyllotoxin(4)and its derivatives we.re reported.Trifluoroacetic acid was used as a condensating agent of 4′-demethylepipodophyllotoxin(5)with 2-mercaptoethylamine without the protection of phenolic hydroxyand amino groups of 5 to give 4.Twenty of title derivatives were screened in vitro.These S-substituted podophyllotoxin derivatives are less active than etoposide andN-substitute derivatives.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
1992年第4期159-162,167,共5页
Chinese Journal of Pharmaceuticals
关键词
鬼臼毒素
衍生物
合成
抗肿瘤活性
podophyllotoxin
derivatives
synthesis
antitumor activities
