3-hydroxymethyl-5-aziridinyl-1-methyl-2-(1H-indole-4,7-dione) prop-beta-en-alpha-ol
[A bioreductive indoloquinone prodrug with potential antineoplastic and radiosensitizing activities. Apaziquone, an analogue of mitomycin C, becomes activated after being reduced by various reductases depending on tissue types. The activated metabolite and the reactive free radicals generated during reduction process cause DNA damages, thereby leading to induction of apoptosis. Furthermore, this agent displays cancer selectivity against both the hypoxic solid tumors, which exhibits higher expression of cytochrome P450 reductase, and also against the well-oxygenated malignant cells that overexpress the bioreductive enzyme NQO1 (NAD(P)H: quinone oxidoreductase). ( NCI )]
UMLS (NCI) C0095568- Organic Chemical
- Pharmacologic Substance
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