Functionalized glycomers as growth inhibitors and inducers of apoptosis in human glioblastoma cells.
The effects of functionalized aryl beta-D-glycopyranosides (glycomers) on the proliferation, survival, and apoptosis of human glioblastoma cells in culture were evaluated as a way to control tumor progression. The results showed that inhibition of growth and/or induction of apoptosis can be achieved by these molecules in human glioblastoma cells. Inhibition of DNA synthesis precedes induction of apoptosis and growth inhibition. The substituents at C-1, C-2, C-3,C-4, and C-6 on the pyranosidic scaffold are important to modulate the action and the efficacy of these molecules. Human fibroblasts and brain-derived endothelial cells were less sensitive to glycomers than tumor cells. Thus, functionalized aryl beta-D-glycopyranosides represent a new class of molecules potentially able to control the progression of brain tumors.
Hanessian
Stephen
S
Department of Chemistry, Université de Montréal, C. P. 6128, Succursale Centre-Ville, Montréal, Province of Quebec, Canada, H3C 3J7. stephen.hanessian@umontreal.ca
Zhan
Lijie
L
Bovey
Raymonde
R
Saavedra
Oscar M
OM
Juillerat-Jeanneret
Lucienne
L
D017209:Apoptosis; D001932:Brain Neoplasms / Q000473:pathology*; D002455:Cell Division / Q000187:drug effects; D002460:Cell Line; D002540:Cerebral Cortex / Q000166:cytology; D004727:Endothelium / Q000166:cytology / Q000187:drug effects; D005347:Fibroblasts / Q000166:cytology / Q000187:drug effects; D005909:Glioblastoma / Q000473:pathology*; D005960:Glucosides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D014407:Tumor Cells, Cultured
D005960:Glucosides