UMYMFOR   05516
UNIDAD DE MICROANALISIS Y METODOS FISICOS EN QUIMICA ORGANICA
Unidad Ejecutora - UE
artículos
Título:
Synthesis and cytotoxic activity evaluation of dihydrocucurbitacin B and cucurbitacin B derivatives
Autor/es:
LANG K. L.; SILVA I.T.; ZIMMERMANN L. A.; ROCHA MACHADO V.; RODRIGUES TEIXEIRA M.; LAPUH M. I.; GALETTI M. A.; PALERMO J. A.; CABRERA G. M.; CAMPOS BERNARDES L. S. ; OLIVEIRA SIMOES C. A.; SCHENKEL E. P.; SORIANO BALPARDA CARO M.; DURAN F. J.
Revista:
BIOORGANIC & MEDICINAL CHEMISTRY.
Editorial:
PERGAMON-ELSEVIER SCIENCE LTD
Referencias:
Lugar: Amsterdam; Año: 2012 vol. 20 p. 3016 - 3030
ISSN:
0968-0896
Resumen:
Two cucrbitacins: dihydrocucurbitacin B (1) and cucurbitacin B (2), which can be obtained in large amounts from the roots of Wilbrandia ebracteata and from the fruits of Luffa opperculata, respectively, were used as starting materials for the preparation of a library of twenty-nine semi-synthetic derivatives. The structural changes that were performed include the removal, modification or permutation of functional groups in rings A and B as well as in the side chain. All new semisynthetic compounds, as well as 1 and 2, were tested in vitro for their cytotoxic effects on non-small-cell lung cancer cells (A549 cells). Some of these compound displayed potent to moderate activity against A549 tumor cells, especially those cucurbitacin B derivatives which were modified at ring A.