Synthesis and antitumour activity of new dendritic polyamines-(imide-DNA-intercalator) conjugates:: potent Lck inhibitors

被引:30
作者
Braña, MF
Domínguez, G
Sáez, B
Romerdahl, C
Robinson, S
Barlozzari, T
机构
[1] Univ San Pablo, CEU, Fac Ciencias Expt & Tecn, Dept Quim Organ & Farmaceut, Madrid 28668, Spain
[2] BASF, Biores Corp, Worcester, MA 01605 USA
关键词
antitumour; dendritic polyamines; intercalators; amides; Lck;
D O I
10.1016/S0223-5234(02)01362-4
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of dendritic polyamines-(imide-DNA-intercalators) conjugates with different connectivity in their basic chain were synthesised and evaluated as antitumour compounds. Although their antiproliferative activity against HT-29 was not significant, conjugates 13 and 16 showed a promising profile as inhibitors of Lck. (C) 2002 Editions scientifiques et medicales Elsevier SAS. All rights reserved.
引用
收藏
页码:541 / 551
页数:11
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