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Bioorg Med Chem ; 20(9): 3016-30, 2012 May 01.
Artículo en Inglés | MEDLINE | ID: mdl-22472043

RESUMEN

Two cucurbitacins, 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 operculata, respectively, were used as starting materials for the preparation of a library of 29 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.


Asunto(s)
Antineoplásicos/síntesis química , Antineoplásicos/toxicidad , Triterpenos/química , Triterpenos/toxicidad , Antineoplásicos/química , Línea Celular Tumoral , Proliferación Celular/efectos de los fármacos , Cucurbitaceae/química , Frutas/química , Humanos , Luffa/química , Raíces de Plantas/química , Triterpenos/síntesis química
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