Chimie Bioorganique et Bioinorganique
1.6. Extraction of natural substances (Gambogic acid, Tagitinin C), synthesis and biological evaluation of derivatives of these natural molecules as new anticancer agents
S. Pethe & G. Vo Thanh (ICMMO/ECM)
Gambogic Acid
- Extracted from the resin of different species of Garcinia. Phase IIA development in China as an anti-cancer agent
- Displays a caged xanthone essential for its anti-cancer activity: pharmacomodulation on the carboxylic acid and the phenol function.
Tagitinine C
-Extracted from Tithonia diversifolia (plant). Used in traditional medicine (diabetes, malaria, hematoma ...).
-From the family of sesquiterpene lactones which have shown anti-cancer activities. Molecule still little studied.
-Pharmacomodulation on the ester, the alcohol function and one of the double bonds of the unsaturated α-β ketone
-Synthesis of analogues for an approach to the total synthesis of Tagitinin C.
For both series of derivatives: biological evaluations on cancer cells and search for the mechanism of action.