Synthesis and antimitotic activity of novel 2-methoxyestradiol analogs

Steroids. 2002 Dec;67(13-14):1079-89. doi: 10.1016/s0039-128x(02)00066-1.

Abstract

The syntheses and antimitotic activity of several novel 2-methoxyestradiol analogs are described. Structural modifications investigated include introduction of additional unsaturation in rings B and D; inversion at C-13; and substitution at the C-2, C-15, C-16, and C-7 alpha positions. Of 15 analogs synthesized, 2 have demonstrated superior biological activities compared to 2-methoxyestradiol.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • 2-Methoxyestradiol
  • Animals
  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Aorta
  • Cell Division / drug effects
  • Cell Line
  • Estradiol / analogs & derivatives
  • Estradiol / chemical synthesis*
  • Estradiol / chemistry
  • Estradiol / pharmacology*
  • Inhibitory Concentration 50
  • Microtubules / drug effects
  • Mitosis / drug effects
  • Molecular Structure
  • Muscle, Smooth, Vascular / cytology
  • Muscle, Smooth, Vascular / drug effects
  • Rats
  • Structure-Activity Relationship

Substances

  • Antineoplastic Agents
  • Estradiol
  • 2-Methoxyestradiol