Synthesis and biological evaluation of cyclic nitrogen mustards based on carnitine framework.
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.
Leiris
Simon
S
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.
Lucas
Marc
M
Dupuy d'Angeac
Arnaud
A
Morère
Alain
A
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D002331:Carnitine / Q000737:chemistry*; D006801:Humans; D020128:Inhibitory Concentration 50; D008928:Mitochondria / Q000187:drug effects / Q000378:metabolism; D009588:Nitrogen Mustard Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
D000970:Antineoplastic Agents; D009588:Nitrogen Mustard Compounds; D002331:Carnitine