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A series of nitroimidazoles containing aziridine and alkyl-substituted aziridine functions has been synthesized. The 2-nitroimidazole compounds examined all show greater radiosensitizing efficiency in vitro than misonidazole. The 4- and 5-nitroimidazole analogues are also more efficient than equivalent compounds which do not contain the alkylating aziridine moiety. All the compounds show increased toxicity towards hypoxic cells relative to aerobic cells, but this toxicity is reduced by alkyl-substitution of the aziridine ring. In vivo toxicity can also be reduced by modification of the aziridine function, but such alterations appear to have less effect upon the high radiosensitizing efficiency of these compounds in vivo. As a consequence of this study, compounds of potentially improved therapeutic utility compared to RSU-1069, the first reported member of this class, have been identified.
I Ahmed, and
T C Jenkins, and
J M Walling, and
I J Stratford, and
P W Sheldon, and
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E M Fielden
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International journal of radiation oncology, biology, physics,
I Ahmed, and
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January 1989,
Cancer chemotherapy and pharmacology,
I Ahmed, and
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British journal of cancer,
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April 1989,
International journal of radiation oncology, biology, physics,
I Ahmed, and
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June 1987,
Biochemical pharmacology,
I Ahmed, and
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May 1984,
British journal of cancer,
I Ahmed, and
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December 1986,
The British journal of radiology,
I Ahmed, and
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I J Stratford, and
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G E Adams, and
E M Fielden
August 1984,
International journal of radiation oncology, biology, physics,
I Ahmed, and
T C Jenkins, and
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I J Stratford, and
P W Sheldon, and
G E Adams, and
E M Fielden
September 1987,
International journal of radiation oncology, biology, physics,
I Ahmed, and
T C Jenkins, and
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I J Stratford, and
P W Sheldon, and
G E Adams, and
E M Fielden
January 1993,
Drug design and discovery,
