Synthesis and antiproliferative activity of A-ring aromatised and conduritol-like steroidal compounds

Steroids. 2005 Dec 15;70(14):922-32. doi: 10.1016/j.steroids.2005.07.001. Epub 2005 Sep 1.

Abstract

A simple approach to aromatization of steroidal quinols and epoxyquinols using a catalytic amount of TMSOTf is reported. Beside acetylation of the angular OH, the acid-catalyzed (TfOH) dienone-phenol rearrangement occurred affording "para" products, or in the case of blocked position 4, the acetoxy group 1,2-migration leads to the formation of "meta" products. Using epoxyquinol derivative as a substrate, the acetoxy group elimination was observed, followed by acid-catalyzed epoxy-ring opening and subsequent double bond migration, giving as a final product Delta(9,11)A-ring aromatized compounds. Synthesis of conduritol-like compounds and structure confirmation by X-ray crystallography of the precursor of steroidal conduritol is also described. In addition, the results of extensive antiproliferative screening against a panel of 60 cancer cell lines are presented.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Catalysis
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Crystallography, X-Ray
  • Cyclohexanols / chemical synthesis*
  • Cyclohexanols / chemistry
  • Cyclohexanols / pharmacology*
  • Cyclohexenes
  • Drug Screening Assays, Antitumor
  • Humans
  • Hydrocarbons, Aromatic / chemical synthesis*
  • Hydrocarbons, Aromatic / chemistry
  • Hydrocarbons, Aromatic / pharmacology*
  • Hydroquinones / chemistry
  • Molecular Structure

Substances

  • Cyclohexanols
  • Cyclohexenes
  • Hydrocarbons, Aromatic
  • Hydroquinones
  • conduritol B