Synthesis of a novel class of cdc25A inhibitors from vitamin D3

Bioorg Med Chem Lett. 2000 Apr 3;10(7):615-7. doi: 10.1016/s0960-894x(00)00065-2.

Abstract

We have developed a novel class of cdc25A inhibitors by drastic modification of the hydrophobic and hydrophilic substructures of dysidiolide. The unsaturated derivative 3b strongly inhibited cdc25A (IC50 = 7.7 microM) and caused GI arrest of HL60 cells.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • 4-Butyrolactone / analogs & derivatives
  • 4-Butyrolactone / chemistry
  • 4-Butyrolactone / pharmacology
  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Cholecalciferol / analogs & derivatives*
  • Cholecalciferol / pharmacology
  • Enzyme Inhibitors / chemical synthesis*
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / pharmacology
  • G1 Phase / drug effects*
  • HL-60 Cells
  • Humans
  • cdc25 Phosphatases / antagonists & inhibitors*

Substances

  • Antineoplastic Agents
  • Enzyme Inhibitors
  • Cholecalciferol
  • CDC25A protein, human
  • cdc25 Phosphatases
  • dysidiolide
  • 4-Butyrolactone