8-甲氧基-15,16-二降-6,8,10-三梭链孢菌三烯12,13α-环氧化物和12,13β-环氧化物作为潜在抗肿瘤药物的合成

Synthesis of 8-methoxy-15,16-dinor-6,8,10-trichothecatriene 12,13 alpha-epoxide and 12,13 beta-epoxide as potential antineoplastic agents.

作者信息

Anderson W K, Lee G E

出版信息

J Med Chem. 1980 Jan;23(1):96-7. doi: 10.1021/jm00175a021.

Abstract

8-Methoxy-15,16-dinor-6,8,10-trichothecatriene 12,13 alpha-epoxide (5) and 12,13 beta-epoxide (3) were prepared; the stereochemistry of the epoxides was assigned on the basis of 13C NMR. The epoxide 5 was active against 9KB in vitro and P388 in vivo, while the isomeric epoxide 3 was inactive in both test systems.

摘要

制备了8-甲氧基-15,16-二降-6,8,10-三烯孢菌素12,13α-环氧化物（5）和12,13β-环氧化物（3）；基于13C核磁共振确定了环氧化物的立体化学。环氧化物5在体外对9KB细胞有活性，在体内对P388细胞有活性，而异构体环氧化物3在这两种测试系统中均无活性。