Antiproliferative activity of 2-alkyl-4-halopiperidines and 2-alkyl-4-halo-1,2,5,6-tetrahydropyridines in solid tumor cell lines

A series of trans-2-alkyl-4-halopiperidines and 2-alkyl-4-halo-1,2,5,6-tetrahydropyridines were prepared by means of an iron(III) catalyzed process. The in vitro antiproliferative activities were examined in the human solid tumor cell lines A2780 (ovarian cancer), SW1573 (non-small cell lung cancer), and WiDr (colon cancer). The results on the biological activity revealed that, in general, the 2-alkyl-4-halo-1,2,5,6-tetrahydropyridine analogs are more potent than the trans-2-alkyl-4-halopiperidine derivatives. A remarkable selectivity of the aza compound 5f for the resistant cell line WiDr was observed. Cell cycle studies revealed a G2/M phase arrest for 5f.

Saved in:
Bibliographic Details
Main Authors: León, Leticia G., Carballo, Rubén M., Vega-Hernández, María C., Martín, Víctor S., Padrón, Juan I., Padrón, José M.
Other Authors: Ministerio de Educación y Ciencia (España)
Format: artículo biblioteca
Language:English
Published: Elsevier 2007-05-17
Subjects:Marine drugs, Anticancer drugs, Halogenated piperidines, Halogenated tetrahydropyridines, Solid tumors, Structure–activity relationship,
Online Access:http://hdl.handle.net/10261/212239
Tags: Add Tag
No Tags, Be the first to tag this record!