Affordable Access

Publisher Website

Synthesis of a novel nitroimidazole-spermidine derivative as a tumor-targeted hypoxia-selective cytotoxin

Authors
Journal
Bioorganic & Medicinal Chemistry Letters
0960-894X
Publisher
Elsevier
Publication Date
Volume
14
Issue
6
Identifiers
DOI: 10.1016/j.bmcl.2003.12.100

Abstract

Abstract A four-step synthesis of ( R,S)- N 4-[3-(2-nitro-1-imidazolyl)-2-hydroxypropyl]-spermidine trihydrochloride ( 4) is described and the utilization of the polyamine active transport system for the uptake of this compound in cells is demonstrated. Thus, V79 cells pretreated with an inhibitor of spermidine biosynthesis, α-difluoromethylornithine (DFMO), are ca. 2-fold more sensitive to 4 under hypoxic conditions, compared to untreated cells. Similarly, radiosensitization of hypoxic V79 cells by 4 is improved in DFMO-pretreated cells.

There are no comments yet on this publication. Be the first to share your thoughts.