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Mini-Reviews in Medicinal Chemistry


ISSN (Print): 1389-5575
ISSN (Online): 1875-5607

Recent Advances in Bioreductive Drug Targeting

Author(s): M. A. Naylor and P. Thomson

Volume 1, Issue 1, 2001

Page: [17 - 29] Pages: 13

DOI: 10.2174/1389557013407241


Advances in the chemistry of bioreductive drug activation have led to the design of hypoxia-selective drug delivery systems. These prodrugs, comprising a bioreductive trigger, linker and effector were first explored with nitrobenzyl quaternary ammonium mustards. Alternative nitroheterocycles were subsequently developed, together with new avenues of prodrug activation in ADEPT and GDEPT. Major advances have also been made in utilising indolequinone reductive chemistry based upon an appreciation of the kinetics of oxygen-sensitive reductive elimination.

Keywords: Bioreductive Drug Targeting, ammonium mustards, cytotoxic chemotherapeutic drugs, radiosensitisers, superoxide radicals, nitrogen atom, diethyl dithiocarbamate, carbamate linker, Bergman cyclisation, nitroimidazole trigger, cyclopropamitosenes

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