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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 08期

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

页码：767 / 770

页数：4

共 19 条

[1] STRUCTURE-ACTIVITY ASPECTS OF HEMICHOLINIUM-3 (HC-3) AND ITS ANALOGS AND CONGENERS [J].