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Bioorg Med Chem ; 10(1): 71-7, 2002 Jan.
Article in English | MEDLINE | ID: mdl-11738608

ABSTRACT

The syntheses and preliminary evaluation of the first potential bioreductive paclitaxel prodrugs are described. These prodrugs were designed as potential candidates in more selective chemotherapy by targeting hypoxic tumour tissue. Aromatic nitro and azide groups were used as the bioreductive trigger. Generation of paclitaxel occurs after reduction and subsequent 1,6-elimination or 1,8-elimination. All prodrugs are stable in buffer and indeed give paclitaxel after chemical reduction of the aromatic nitro or azide functionality. In aerobic cytotoxicity assays several prodrugs exhibit diminished cytotoxicity. These compounds are interesting candidates for further biological evaluation.


Subject(s)
Antineoplastic Agents/chemistry , Paclitaxel/chemistry , Prodrugs/chemical synthesis , Prodrugs/pharmacokinetics , Antineoplastic Agents/chemical synthesis , Antineoplastic Agents/pharmacokinetics , Cell Division/drug effects , Humans , Magnetic Resonance Spectroscopy , Oxidation-Reduction , Prodrugs/pharmacology , Spectrum Analysis , Tumor Cells, Cultured
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