Synthesis, biological activity, and conformational analysis of CD-ring modified trans-decalin 1 alpha,25-dihydroxyvitamin D analogs

Org Biomol Chem. 2003 Jan 21;1(2):257-67. doi: 10.1039/b209147j.

Abstract

A novel series of analogs of 1,25-dihydroxyvitamin D3, the hormonally active metabolite of vitamin D3, characterised by the presence of a trans-fused decalin CD-ring system, possesses surprising biological activities in combination with specific structural modifications in the flexible parts of the molecule, when compared with the natural hydrindane derivatives. (1) A large difference in biological activity is observed between the 20-epimeric trans-decalin analogs that follows a pattern opposite to what is usually observed for the natural ring size. (2) Several trans-decalin analogs that are modified in the seco-B-ring region, including previtamin derivatives, possess a pronounced vitamin D-like activity, whereas the corresponding hydrindane derivatives are inactive. The molecular origin of this behavior is still under study.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Breast Neoplasms / metabolism
  • Calcitriol / analogs & derivatives*
  • Calcitriol / chemical synthesis
  • Calcitriol / metabolism*
  • Calcitriol / pharmacology*
  • Calcium / blood
  • Cell Differentiation / drug effects
  • Cell Division / drug effects
  • Cell Line, Tumor
  • HL-60 Cells
  • Humans
  • Keratinocytes / drug effects
  • Mice
  • Models, Molecular
  • Molecular Conformation
  • Naphthalenes / chemistry*
  • Naphthalenes / metabolism
  • Naphthalenes / pharmacology
  • Receptors, Calcitriol / metabolism
  • Stereoisomerism
  • Structure-Activity Relationship
  • Swine
  • Vitamin D-Binding Protein / metabolism

Substances

  • Naphthalenes
  • Receptors, Calcitriol
  • Vitamin D-Binding Protein
  • decalin
  • Calcitriol
  • Calcium