Synthesis and biological evaluation of new 5-fluorouracil-substituted ampelopsin derivatives

Molecules. 2010 Mar 24;15(4):2114-23. doi: 10.3390/molecules15042114.

Abstract

This study reports two novel 5-fluorouracil-substituted ampelopsin derivatives. The structures of two new derivatives were characterized by elemental analysis, 1H-NMR, 13C-NMR, IR and MS. Their anticancer activities in vitro against two cancer cell lines, K562 and K562/ADR, were investigated using the MTT assay, and the results showed that the two new compounds were more effective than reference drugs such as ampelopsin and verapamil.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology
  • Cell Line, Tumor
  • Flavanones / chemical synthesis*
  • Flavanones / chemistry
  • Flavanones / pharmacology
  • Flavonoids / chemical synthesis*
  • Flavonoids / chemistry*
  • Flavonoids / pharmacology
  • Fluorouracil / analogs & derivatives*
  • Fluorouracil / chemical synthesis
  • Fluorouracil / chemistry*
  • Fluorouracil / pharmacology
  • Humans

Substances

  • 2-(4-(2-(5-fluoro-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)acetoxy)-3,5-dihydroxyphenyl)-5,7-dihydroxy-4-oxochroman-3-yl-2-(5-fluoro-2-dihydropyrimidin-1(2H)-yl)acetate
  • 5,7-dihydroxy-4-oxo-2-(3,4,5-trihydroxyphenyl)chroman-3-yl-2-(5-fluoro-2,4-dioxo-3,4-dihydroxypyrimidin-1(2H)-yl)acetate
  • Antineoplastic Agents
  • Flavanones
  • Flavonoids
  • ampelopsin
  • Fluorouracil