STRUCTURE-ACTIVITY RELATIONSHIP OF ALPHA-GALACTOSYLCERAMIDES AGAINST B16-BEARING MICE

被引：507

作者：

MORITA, M ^{[1
]}

MOTOKI, K ^{[1
]}

AKIMOTO, K ^{[1
]}

NATORI, T ^{[1
]}

SAKAI, T ^{[1
]}

SAWA, E ^{[1
]}

YAMAJI, K ^{[1
]}

KOEZUKA, Y ^{[1
]}

KOBAYASHI, E ^{[1
]}

FUKUSHIMA, H ^{[1
]}

机构：

[1] KIRIN BREWERY CO LTD,PHARMACEUT RES LAB,TAKASAKI,GUMMA 37012,JAPAN

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1995年 / 38卷 / 12期

关键词：

D O I：

10.1021/jm00012a018

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Agelasphin-9b, (2S,3S,4R)-1-O-(alpha-D-galactopyranosyl)-16-methyl-2-[N-((R)-2-hydroxytetracosanoyl)-amino]-1,3,4-heptadecanetriol, is a potent antitumor agent isolated from the marine sponge Agelas mauritianus. Various analogues of agelasphin-9b (a lead compound) were synthesized, and the relationship between their structures and biological activities was examined using several assay systems. From the results, KRN7000, (2S,3S;4R)-1-O-(alpha-D-galactopyranosyl)2-(N-hexacosanoylamino)-1,3,4-octadecanetriol, was selected as a candidate for clinical application.

引用

页码：2176 / 2187

页数：12

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