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

M Morita, K Motoki, K Akimoto, T Natori… - Journal of medicinal …, 1995 - ACS Publications
M Morita, K Motoki, K Akimoto, T Natori, T Sakai, E Sawa, K Yamaji, Y Koezuka, E Kobayashi…
Journal of medicinal chemistry, 1995ACS Publications
Agelasphin-9b,(2S, 3S, 4ñ)-l-0-(aD-galactopyranosyl)-16-methyl-2-[Af-((. 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,
4ñ)-l-0-(aD-galactopyranosyl)-2-üV-hexacosanoylamino)-l, 3, 4-octadecanetriol, was …
Agelasphin-9b,(2S, 3S, 4ñ)-l-0-(aD-galactopyranosyl)-16-methyl-2-[Af-((. 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, 4ñ)-l-0-(aD-galactopyranosyl)-2-üV-hexacosanoylamino)-l, 3, 4-octadecanetriol, was selected as a candidate for clinical ap-plication.
ACS Publications