Influence of the linker in bispyridium compounds on the inhibition of human choline kinase

  • J Med Chem. 2004 Oct 21;47(22):5433-40. doi: 10.1021/jm0496537.
Ana Conejo-García  1 ,  Mónica Báñez-Coronel ,  Rosario M Sánchez-Martín ,  Agustín Rodríguez-González ,  Angeles Ramos ,  Ana Ramírez de Molina ,  Antonio Espinosa ,  Miguel Angel Gallo ,  Joaquín M Campos ,  Juan Carlos Lacal
Affiliations
  • 1. Departamento de Quimica Farmaceutica y Organica, Facultad de Farmacia, Universidad de Grenada, Campus de Cartuja s/n, 18071 Granada, Spain.
PMID: 15481981 DOI: 10.1021/jm0496537
Abstract

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.

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