Influence of the linker in bispyridium compounds on the inhibition of human choline kinase.
Basic Information
ID: ALA1138794
Journal: J Med Chem
Title: Influence of the linker in bispyridium compounds on the inhibition of human choline kinase.
Authors: Conejo-García A, Báñez-Coronel M, Sánchez-Martín RM, Rodríguez-González A, Ramos A, Ramírez de Molina A, Espinosa A, Gallo MA, Campos JM, Lacal JC.
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.
CiteXplore: 15481981
DOI: 10.1021/jm0496537
Patent ID: ┄