Cytotoxic Activity of Semi-Synthetic Derivatives of Elatol and Isoobtusol

Marine Drugs

Karen L. Lang¹  Izabella T. Silva¹  Lara A. Zimmermann¹  Cíntia Lhullier¹  Maria V. Ma༚lich Arana²  Jorge A. Palermo²  Miriam Falkenberg¹  Cláudia M. O. Simཞs¹  Eloir P. Schenkel¹ 

[1] Department of Pharmaceutical Sciences, Federal University of Santa Catarina, Florianópolis, SC, 88040-970, Brazil;Department of Organic Chemistry, University of Buenos Aires, Buenos Aires, C1428EGA, Argentina;

关键词: elatol;    isoobtusol;    sesquiterpenes;    synthesis;    cytotoxic activity;   

DOI  :  10.3390/md10102254

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
© 2012 by the authors; licensee MDPI, Basel, Switzerland.