Abstract
We proposed a strategy of photooxidizer-reduction activated alkylator (P-A) hybrid molecule to develop novel oxygen-independent photosensitizers. Two prototypes of such photosensitizers camptothecin-indolequinone (CPT-IQ) and camptothecin-nitrofuryl (CPT-NF) was designed and prepared. A mechanism of photo-induced oxidation and alkylation of 2'-deoxyguanosine by CPT-IQ was investigated. CPT-NF was confirmed to effectively induce DNA cleavage via 365-nm UV irradiation both under normaxia and hypoxia.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Alkylation
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Anaerobiosis
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Camptothecin / analogs & derivatives*
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Camptothecin / chemical synthesis
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Camptothecin / chemistry
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Camptothecin / radiation effects
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Deoxyguanosine / chemistry
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Furans / chemical synthesis
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Furans / chemistry*
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Furans / radiation effects
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Oxidation-Reduction
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Photosensitizing Agents / chemical synthesis
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Photosensitizing Agents / chemistry*
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Photosensitizing Agents / radiation effects
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Quinones / chemical synthesis
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Quinones / chemistry*
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Quinones / radiation effects
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Ultraviolet Rays
Substances
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4-deshydroxy-4-(N-methyl-(2-(((5-methoxy-1,2-dimethyl-4,7-dioxoindol-3-yl)methoxycarbonyl)(methyl)amino)ethyl)carbamoylmethyl)camptothecin
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4-deshydroxy-4-(N-methyl-(2-(((5-nitrofur-2-yl)methoxycarbonyl)(methyl)amino)ethyl)carbamoylmethyl)camptothecin
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Furans
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Photosensitizing Agents
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Quinones
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Deoxyguanosine
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Camptothecin