Novel A-ring analogs of the hormone 1alpha,25-dihydroxyvitamin D3: synthesis and preliminary biological evaluation

Bioorg Med Chem. 2005 Apr 15;13(8):2959-66. doi: 10.1016/j.bmc.2005.02.005.

Abstract

Prepared from a commercial prostaglandin building block, novel vitamin D3 analogs with a contracted five-membered A-ring were designed and synthesized to mimic the A-ring diol structure of the natural hormone 1alpha,25-dihydroxyvitamin D3. Prepared from commercial 1,4-cyclohexanedione, a structurally simplified analog was designed and synthesized in which a suitably oriented primary allylic hydroxyl group at the C-2 position might be a surrogate for the biologically important 1alpha-OH in the natural hormone.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Animals
  • COS Cells
  • Cell Proliferation / drug effects
  • Cells, Cultured
  • Chlorocebus aethiops
  • Humans
  • Keratinocytes / drug effects
  • Structure-Activity Relationship
  • Vitamin D / analogs & derivatives*
  • Vitamin D / chemical synthesis
  • Vitamin D / chemistry
  • Vitamin D / pharmacology

Substances

  • 2-methyl-1,25-dihydroxyvitamin D3
  • Vitamin D