Synthesis of new Targretin analogues that induce apoptosis in leukemia HL-60 cells

Bioorg Med Chem Lett. 2002 Dec 16;12(24):3529-32. doi: 10.1016/s0960-894x(02)00803-x.

Abstract

Four new analogues of Targretin where the carboxylic acid function was replaced by an N,N-dimethyl-S-aryl carbamate or N,N-dimethyl-O-arylthiocarbamate function, were synthesized. Compounds 5, 6 and 7 have shown to be more potent than the parent compound to induce apoptosis of HL-60 cells.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anticarcinogenic Agents / chemical synthesis*
  • Anticarcinogenic Agents / pharmacology
  • Apoptosis / drug effects*
  • Bexarotene
  • Carbamates / chemical synthesis
  • Carbamates / pharmacology
  • HL-60 Cells
  • Humans
  • Leukemia / pathology*
  • Receptors, Retinoic Acid / agonists
  • Retinoid X Receptors
  • Structure-Activity Relationship
  • Tetrahydronaphthalenes / chemical synthesis*
  • Tetrahydronaphthalenes / pharmacology
  • Transcription Factors / agonists

Substances

  • Anticarcinogenic Agents
  • Carbamates
  • Receptors, Retinoic Acid
  • Retinoid X Receptors
  • Tetrahydronaphthalenes
  • Transcription Factors
  • Bexarotene