Abstract:
:The synthesis and biological activities of four novel bispyridinium cyclophanes as choline kinase (ChoK) inhibitors are presented. Their synthetic methodology has been optimized according to dilution, temperature, and reaction time and provides pure bispyridinium cyclophanes in high yields very easily. One of these cyclophanes (6, 4,8-diaza-3(1,4),9(4,1)-dipyridina-1(1,4),6(1,3)-dibenzenacyclodecaphan-3(1),9(1)-bis(ilium) dibromide) has an IC(50(ChoK)) of 0.3 microM and is the most potent human ChoK inhibitor described to date.
journal_name
J Med Chemjournal_title
Journal of medicinal chemistryauthors
Conejo-García A,Campos JM,Sánchez-Martín RM,Gallo MA,Espinosa Adoi
10.1021/jm030792ikeywords:
subject
Has Abstractpub_date
2003-08-14 00:00:00pages
3754-7issue
17eissn
0022-2623issn
1520-4804journal_volume
46pub_type
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