Abstract
A series of unsymmetrical polar disulfide prodrugs 2-5 of paclitaxel were designed and synthesized as reductively activated prodrugs. These compounds behaved as prodrugs in vitro on L2987 lung carcinoma cells. In vivo evaluation in mice demonstrated that the mutual prodrug 5 with captopril exhibited significant regressions and cures.
MeSH terms
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Animals
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Cell Division / drug effects
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Disulfides
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Dithiothreitol / pharmacology
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Half-Life
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Humans
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Inhibitory Concentration 50
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Mice
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Mice, Nude
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Neoplasms, Experimental / drug therapy
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Oxidation-Reduction
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Paclitaxel
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Prodrugs / chemical synthesis
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Prodrugs / metabolism*
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Prodrugs / pharmacology
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Treatment Outcome
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Tumor Cells, Cultured
Substances
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Disulfides
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Prodrugs
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Paclitaxel
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Dithiothreitol