Synthesis and biological evaluation of nitrogen mustard derivatives of purine bases.

Benjamin Boëns (1) , Mounir Azouz , Tan-Sothea Ouk (1) , Rachida Zerrouki (1)

1 LCSN - Laboratoire de Chimie des Substances Naturelles

This paper deals with the synthesis of nitrogen mustard analogs, derivatives of purine bases. Alkylation in position N-9 and diethanolamine fixation on position 6 were managed by microwave irradiations. Chlorination of these dihydroxylated intermediates led to a cyclization, giving tricyclic purine base analogs bearing a chloroethyl chain. Finally, MTT assays on obtained compounds do not show cytotoxicity on four different cancer cell lines.

Domaines: Chimie organique

Benjamin Boëns, Mounir Azouz, Tan-Sothea Ouk, Rachida Zerrouki. Synthesis and biological evaluation of nitrogen mustard derivatives of purine bases.. Nucleosides, Nucleotides and Nucleic Acids, 2013, 32 (2), pp.69-80. ⟨10.1080/15257770.2013.763977⟩. ⟨hal-00926274⟩