QSAR of 1,1′(1,2-ethylenebisbenzyl)bis(4-substitutedpyridinium) dibromides as choline kinase inhibitors:: a different approach for antiproliferative drug design

被引:30
作者
Campos, J [1 ]
Núñez, MD [1 ]
Rodríguez, V [1 ]
Gallo, MA [1 ]
Espinosa, A [1 ]
机构
[1] Fac Farm, Dept Quim Organ, Granada 18071, Spain
关键词
D O I
10.1016/S0960-894X(00)00080-9
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
XTen new structures of a series of the title compounds were synthesized and screened for their activity to inhibit choline kinase under ex vivo conditions. Their inhibitory potency correlates with the C-13 chemical shifts (in CD3OD) of the methylene group bearing the positively charged nitrogen. The inhibitory effect on proliferation against the HT-29 cell line is strongly dependent on its ability to inhibit the production of phosphorylcholine. (C) 2000 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:767 / 770
页数:4
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