Recent advances in the chemistry and biological activities of canthin-6-one analogs

In the course of our program aiming at the synthesis of analogs of canthin-6-one [1], we present new synthetic developments including new reactivity studies in the indole series. Canthin-6-one type alkaloids are mainly found in the Rutaceae and Simaroubaceae families and have been shown to possess a wide range of biological activities. Among others, we are currently interested in their potent antifungal properties.

Starting from tryptamines and succinic-type anhydrides, a simple and scalable synthetic pathway has been developed for the synthesis of canthin-6-one and analogs.

1. Soriano-Agatón, F. et al. (2005)J. Nat. Prod. 68: 1581–1587.

2. Lagoutte, D. et al. (2008) Biomed Pharmacother 62: 99–103.