2. Academic Validation
  3. Synthesis and biological evaluation of cyclic nitrogen mustards based on carnitine framework

Synthesis and biological evaluation of cyclic nitrogen mustards based on carnitine framework

  • Eur J Med Chem. 2010 Sep;45(9):4140-8. doi: 10.1016/j.ejmech.2010.06.003.
Simon Leiris 1,  Marc Lucas,  Arnaud Dupuy d'Angeac,  Alain Morère
Affiliations

Affiliation

  • 1 Institut des Biomolécules Max Mousseron, UMR 5247, CNRS, Université Montpellier 2 et 1, Bâtiment de Recherche Max Mousseron, Ecole Nationale Supérieure de Chimie de Montpellier, 8 Rue de l'Ecole Normale, F-34296 Montpellier Cedex 05, France.
PMID: 20615582 DOI: 10.1016/j.ejmech.2010.06.003
Abstract

Two series of cyclic nitrogen mustards structurally related to L-carnitine have been prepared. The cytotoxic activity of these compounds was evaluated by using Chlorambucil as a reference. In accordance with earlier report, the cytotoxicity is in direct correlation with the lipophilicity of the introduced alkyl chains. Among the cyclic nitrogen mustards synthesized, the most cytotoxic compounds were the one acylated with a palmitoyl side chain, which showed activities comparable to that of Chlorambucil.

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