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À propos de : Influence of the Linker in Bispyridium Compounds on the Inhibition of HumanCholine Kinase        

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  • Influence of the Linker in Bispyridium Compounds on the Inhibition of HumanCholine Kinase
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  • Studies have been aimed to establish the structure−activity relationship that define cholinekinase (ChoK) inhibitory potency and antiproliferative activity of a set of 25 bispyridiniumcompounds with electron-releasing groups at position 4. Here we report that, according to theirinhibitory activities against human ChoK, the enzymatic inhibitory potency is closely relatedto the size of the linker, the 3,3‘-biphenyl moiety being the most suitable. The N-methylanilinoand its derivatives, 4-chloro-N-methylanilino and 3,5-dichloro-N-methylanilino, render higherChoK inhibitory and antiproliferative activities against the HT-29 human colon cancer cellline.
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