Polyamine transport inhibitors

Drug – bio-affecting and body treating compositions – Solid synthetic organic polymer as designated organic active... – Aftertreated polymer

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Other Related Categories

424 7837, 424 7835, A61K 3174, A61K 31785, A61K 31765

Type

Patent

Status

active

Patent number

06083496&

Description

ABSTRACT:
Described herein are novel specific, pure competitive inhibitors of natural polyamine transport in mammalian cells. Despite their low molecular weight, the inhibitors of the present invention stay virtually impermeant to the cell and display minor non-specific effects while exhibiting a very high affinity for the carrier. More specifically described are synthetic derivatives of original polyamines, wherein the original polyamine is modified to comprise an amido group immediately linked to the polyamine backbone. A side chain may be anchored to the amido group and provide for the formation of dimeric synthetic derivatives or its labelling and subsequent usage as a marker for the polyamine transporter. The use of such novel inhibitors of polyamine transport to evaluate the antitumor efficacy of polyamine depletion strategies with minimal systemic cytotoxic effects or to control and treat disorders involving unrestrained cell proliferation and/or cell differentiation wherein polyamine transport is required as well as pharmaceutical composition thereof are also described.

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