Synthesis of spermidine and norspermidine dimers as high affinity polyamine transport inhibitors

被引:26
|
作者
Covassin, L
Desjardins, M
Charest-Gaudreault, R
Audette, M
Bonneau, MJ
Poulin, R [1 ]
机构
[1] Univ Laval, Fac Med, Dept Physiol, Quebec City, PQ G1K 7P4, Canada
[2] Univ Laval, Fac Pharm, Quebec City, PQ G1K 7P4, Canada
[3] Univ Laval, Fac Med, Dept Pharmacol, Quebec City, PQ G1K 7P4, Canada
[4] Univ Laval, Fac Med, Dept Med Biol, Quebec City, PQ G1K 7P4, Canada
[5] CHUQ, St Francois Assise Hosp, Res Ctr, Quebec City, PQ G1L 3L5, Canada
[6] Univ Laval, Med Res Ctr, CHUQ, Mol Endocrinol Lab, Quebec City, PQ G1V 4G2, Canada
关键词
D O I
10.1016/S0960-894X(99)00262-0
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of novel spermidine and sym-norspermidine dimers was synthesized by crosslinking the polyamine backbones via alkylation of their secondary amino groups to butyl, trans-2-butenyl, 2-butynyl or p-xylyl bridges. The resulting hexamines behaved as high-affinity antagonists of polyamine uptake, with a relative potency that was dependent on the geometry of the linker structure. (C) 1999 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:1709 / 1714
页数:6
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