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J Med Chem. 1995 Jun 9;38(12):2176-87.

Structure-activity relationship of alpha-galactosylceramides against B16-bearing mice.

Author information

1
Pharmaceutical Research Laboratory, Kirin Brewery Company, Ltd., Gunma, Japan.

Abstract

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.

PMID:
7783149
DOI:
10.1021/jm00012a018
[Indexed for MEDLINE]

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