Cytotoxic Activity of Semi-Synthetic Derivatives of Elatol and Isoobtusol

• Main Authors: Eloir P. Schenkel, Fernando J. Durán, Cláudia M. O. Simões, Miriam Falkenberg, Jorge A. Palermo, Maria V. Mañalich Arana, Cíntia Lhullier, Izabella T. Silva, Lara A. Zimmermann, Karen L. Lang
• Format: Article
• Language: English
• Published: MDPI AG 2012-10-01
• Series: Marine Drugs
• Subjects: elatol; isoobtusol; sesquiterpenes; synthesis; cytotoxic activity
• Online Access: http://www.mdpi.com/1660-3397/10/10/2254

In the present study, the in vitro cytotoxic effects of six semi-synthetic derivatives of elatol (1) and isoobtusol (2) were investigated. Chemical modifications were performed on the hydroxyl groups aiming to get derivatives of different polarity, namely the hemisuccinate, carbamate and sulfamate. The structural elucidation of the new derivatives was based on detailed NMR and MS spectroscopic analyses. The in vitro cytotoxicity of compounds 1 to 8 was evaluated against A459 and RD tumor cell lines with CC50 values ranging from 4.93 to 41.53 µM. These results suggest that the structural modifications performed on both compounds could be considered a good strategy to obtain more active derivatives.