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Modifying rates of reductive elimination of leaving groups from indolequinone prodrugs: a key factor in controlling hypoxia-selective drug release.

Abstract:

3-(4-Methylcoumarin-7-yloxy)methylindole-4,7-diones were synthesised as model prodrugs in order to investigate the correlation between rates of reductive elimination from the (indolyl-3-yl)methyl position with reductive metabolism by hypoxic tumor cells and NADPH: cytochrome P450. Rates of elimination of the chromophore/fluorophore (7-hydroxy-4-methylcoumarin) following one-electron reduction of indolequinones to their semiquinone radicals (Q*-) was measured by pulse radiolysis utilising spec...

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Publication status:
Published

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Journal:
Biochemical pharmacology
Volume:
63
Issue:
9
Pages:
1629-1639
Publication date:
2002-05-05
DOI:
EISSN:
1873-2968
ISSN:
0006-2952
URN:
uuid:a612cbce-502b-4831-b9e7-c0148a23250f
Source identifiers:
130873
Local pid:
pubs:130873

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