Preparation and biological activity of 13-substituted retinoic acids

Bioorg Med Chem. 2004 Jul 15;12(14):3931-42. doi: 10.1016/j.bmc.2004.04.047.

Abstract

13-Demethyl or 13-substituted all-E- and 9Z-retinoic acids were synthesized using a palladium-catalyzed coupling reaction of enol triflates and tributylstannylolefins. Their biological activities were then measured. The 13-ethyl analogs exhibited approximately one-half of the antiproliferative and differentiation-inducing activity of ATRA in HL-60 cells. In contrast, in the 9Z-derivatives, all analogs, except for the 13-butyl derivatives, showed apoptosis-inducing activity.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cell Line, Tumor
  • Flow Cytometry
  • Humans
  • Spectrum Analysis
  • Tretinoin / analogs & derivatives
  • Tretinoin / chemical synthesis*
  • Tretinoin / pharmacology*

Substances

  • Tretinoin