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Harmine derivatives

Synthesis, physicochemical characterization, biological and pharmaceutical evaluation of harmine derivatives as anticancer compounds

harmine approach


Harmine is a natural compound presenting anticancer activity. In order to improve harmine anticancer activity, several derivatives of harmine compounds have been synthesized. The physicochemical (solubility, lipophilicity) and biological (MTT test) properties of these compouds were determined. In order to design molecules including the best properties, theoretical models (3D-QSAR) are also developed. Moreover, toxicity of compounds with interesting properties is investigated by in in vitro and in vivo model.

This project is financially supported by Télévie – FNRS


Major steps:

  • Synthesis of harmine derivatives
  • Development of theoretical model (3D-QSAR) allowing to predict best compounds
  • Physicochemical characterization (solubility determination, plasma stability evaluation) using LC analyses
  • Biological characterization on cells (in vitro models)
  • Toxicity evaluation (in vivo model)

Associated references:

Raphaël Frédérick and others, ‘Novel Trisubstituted Harmine Derivatives with Original in Vitro Anticancer Activity.’, Journal of medicinal chemistry, 55 (2012), 6489–501.


Université Libre de Bruxelles, Faculty of Pharmacy, Toxicology Laboratory