Differentiation-inducing activity of retinoic acid isomers and their oxidized analogs on human promyelocytic leukemia HL-60 cells

Biochem Biophys Res Commun. 1992 Dec 15;189(2):1136-42. doi: 10.1016/0006-291x(92)92322-o.


Retinoidal activity of retinoic acid isomers [all-trans-retinoic acid (ATRA), 9-cis-retinoic acid (9CRA) and 13-cis-retinoic acid (13CRA)] and their oxidized derivatives [19-hydroxy and 19-oxo derivatives of ATRA (19-hydroxy-ATRA and 19-oxo-ATRA), 19-oxo derivative of 9CRA (19-oxo-9CRA), and 19-hydroxy derivative of 13CRA (19-hydroxy-13CRA)] was evaluated by means of a human promyelocytic leukemia HL-60 cell differentiation induction assay. All the compounds examined showed this activity with ED50 values of 2-30 nM, which are in accordance with their binding activity to nuclear retinoic acid receptors (RARs).

MeSH terms

  • Binding, Competitive
  • Carrier Proteins / metabolism
  • Cell Differentiation / drug effects*
  • Dose-Response Relationship, Drug
  • Humans
  • Isomerism
  • Leukemia, Promyelocytic, Acute
  • Molecular Structure
  • Oxidation-Reduction
  • Receptors, Retinoic Acid
  • Structure-Activity Relationship
  • Tretinoin / analogs & derivatives*
  • Tretinoin / metabolism
  • Tretinoin / pharmacology*
  • Tumor Cells, Cultured


  • Carrier Proteins
  • Receptors, Retinoic Acid
  • Tretinoin