Synthesis and biological evaluation of O-alkylated tropolones and related alpha-ketohydroxy derivatives as ribonucleotide reductase inhibitors

A series of O-alkylated tropolones and related alpha -ketohydroxy compounds were evaluated for their biological activities and were shown to present a n expected ribonucleotide reductase inhibition and cytotoxicity against som e cancer cell lines but no antitubulin activity. Pharmacomodulation studies were realised to understand and enhance the observed activities. These ori ginal benzylic, heterocyclic and allylic compounds have been synthesised by a phase-transfer catalysed O-alkylation developed in our laboratories. (C) 2001 Editions scientifiques et medicales Elsevier SAS.