Bioorganic & Medicinal Chemistry Letters 2003-10-06

Xylylated dimers of putrescine and polyamines: influence of the polyamine backbone on spermidine transport inhibition.

Laurence Covassin, Michel Desjardins, Denis Soulet, René Charest-Gaudreault, Marie Audette, Richard Poulin

Index: Bioorg. Med. Chem. Lett. 13(19) , 3267-71, (2003)

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Abstract

Dimeric norspermidine and spermidine derivatives are strong competitive inhibitors of polyamine transport. A xylyl tether was used for the dimerization of various triamines and spermine via a secondary amino group, and of putrescine via an ether or an amino group. Dimerization of putrescine moieties potentiates their ability to compete against spermidine transport to a much greater extent than for triamine dimers.