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tested in murine L1210 leukemic cells, fully acetylated 6-fluoro-ManNAc had an IC50 value of 100 ^M, 6-fluoro-ManN had an IC50 value of 1 mM, and 6-fluoro-ManNAc was inactive (Table 6). The 3-fluoro analogs both inhibited cell growth at micromolar concentrations and reduced tumor growth by 50%. The 3-fluoro GlcNAc derivative also appeared to inhibit glycoconjugate biosynthesis. In the presence of the 3-fluoro analog, incorporation of [3H]GlcN was reduced by 41% and [3H]thymidine by only 7%. This indicates that 3-fluoro-GlcNAc competes in the

Table 5 Growth Inhibitory Activity of Various Halogenated Gal Derivatives Against L1210 Leukemia Cells

H0^biroH

Table 6 Growth Inhibitory Activity of Various ManNAc, GlcNAc, and GalNAc Derivatives Against L1210 Leukemia Cells

Table 6 Growth Inhibitory Activity of Various ManNAc, GlcNAc, and GalNAc Derivatives Against L1210 Leukemia Cells

ManN GlcN GaIN

ManN GlcN GaIN

IC5o (mM)

Ri

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