摘要
根据鬼臼毒素类化合物C_4位氮取代衍生物构效原理,设计并合成了11个4-取代氨基或烃氧甲酰胺基表鬼臼毒素类似物。从鬼臼毒素出发,经溴代、水解、叠氮化、还原以及酰化等六步反应合成标题化合物。体外抗肿瘤活性试验表明这类化合物具有较为显著的生物活性,多数化合物对L1210白血病肿瘤细胞与KB细胞生长抑制活性超过临床用药依托泊甙。
A series of 4-substituted formamylamido-4-deoxy-4′-demethylepipodophyllotoxins were synthesized in six steps, and evaluated for their inhibitory activity against L1210 leukemia and KB cells (in vitro). These compounds exhibited remarkable antitumor activity and are more potent than etoposide(VP-16-213).
出处
《中国药科大学学报》
CAS
CSCD
北大核心
1993年第3期134-138,共5页
Journal of China Pharmaceutical University
关键词
鬼臼毒素
抗肿瘤活性
合成
Podophyllotoxin
4-Substituted formamylamido-4-deoxy-4'-demethylepipodophyllotoxin analogues
Antitumor activity
