INTEQUI   20941
INSTITUTO DE INVESTIGACIONES EN TECNOLOGIA QUIMICA
Unidad Ejecutora - UE
artículos
Título:
Derivatives of grindelic acid: From a non-active natural diterpene to synthetic antitumor derivatives
Autor/es:
RETA, G.F.; CHIARAMELLO, A.; GARCÍA, C.; LEÓN, L.G.; MARTÍN, V.S.; PADRÓN, J.M.; TONN, C.E.; DONADEL, O.J.
Revista:
EUROPEAN JOURNAL OF MEDICAL CHEMISTRY
Editorial:
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
Referencias:
Lugar: Paris; Año: 2013 vol. 67 p. 28 - 38
ISSN:
0223-5234
Resumen:
Using several reactions that include homologations and asymmetric epoxidations as well as Ugi and Huisgen couplings, we generated a small focused library of new derivatives from the labdane-type diterpene grindelic acid. These compounds were evaluated as cytotoxic agents against a panel of five human solid tumor cell lines (HBL-100, HeLa, SW1573, T-47D, and WiDr). The presence of the diamide functionalizations enhanced the cytotoxic effect. N-Benzyl-N-(1-(benzylamino)-2-methyl-1-oxopropan- 2-yl)grindelicamide, proved to be the most active product in all cell lines tested, with values of 0.95 (0.38) mM against HBL-100 cells.