摘要
合成了4-脱氧-4-磺酰胺基-4′-去甲表鬼臼毒素衍生物25个。在抑制 L1210白血病细胞和 KB 细胞的试验中,大部分磺酰胺基表鬼臼毒素显示比依托泊甙更强的活性。简要讨论了该类化合物的结构-活性关系。
4-Deoxy-4-sulfonylamino-4'-demethylepipophyllotoxins were syn-thesized from 4-amino-4-deoxy-4'-demethylepipodophyllotoxin and aliphatic or aro-matic sulfonyl chlorides in the presence of Et_3N.Among of the 25 new com-pounds,some O-methylphenylsulfonylamino and halogen-substituted aromatic sul-fonylaminopodophyllotoxins showed the remarkable antitumor activity againstL1210 leukemia cells than that of etoposide.The structure activity relationshipis briefly discussed.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
1993年第5期198-201,共4页
Chinese Journal of Pharmaceuticals
关键词
表鬼臼毒素
合成
抗肿瘤活性
4'-demethylepipodophyllotoxin
podophyllotoxin
4-deoxy-4-sulfonylamino-4'-demethylepipodophyllotoxin
synthesis
antitumor
