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Influence of the Linker in Bispyridium Compounds on the Inhibition of Human Choline Kinase

2004; American Chemical Society; Volume: 47; Issue: 22 Linguagem: Inglês

10.1021/jm0496537

1520-4804

Ana Conejo‐García, Mónica Báñez-Coronel, Rosario M. Sánchez‐Martín, Agustı́n Rodrı́guez-González, A. C. RAMOS, Ana Ramı́rez de Molina, Antonio Espinosa, Miguel Á. Gallo, Joaquín M. Campos Rosa, Juan Carlos Lacal,

Retinoids in leukemia and cellular processes

Studies have been aimed to establish the structure−activity relationship that define choline kinase (ChoK) inhibitory potency and antiproliferative activity of a set of 25 bispyridinium compounds with electron-releasing groups at position 4. Here we report that, according to their inhibitory activities against human ChoK, the enzymatic inhibitory potency is closely related to the size of the linker, the 3,3'-biphenyl moiety being the most suitable. The N-methylanilino and its derivatives, 4-chloro-N-methylanilino and 3,5-dichloro-N-methylanilino, render higher ChoK inhibitory and antiproliferative activities against the HT-29 human colon cancer cell line.