Functionalized glycomers as growth inhibitors and inducers of apoptosis in human glioblastoma cells

J Med Chem. 2003 Aug 14;46(17):3600-11. doi: 10.1021/jm0205853.

Abstract

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Apoptosis*
  • Brain Neoplasms / pathology*
  • Cell Division / drug effects
  • Cell Line
  • Cerebral Cortex / cytology
  • Endothelium / cytology
  • Endothelium / drug effects
  • Fibroblasts / cytology
  • Fibroblasts / drug effects
  • Glioblastoma / pathology*
  • Glucosides / chemical synthesis*
  • Glucosides / chemistry
  • Glucosides / pharmacology
  • Humans
  • Tumor Cells, Cultured

Substances

  • Glucosides