Synthesis of 6-O-methotrexylhyaluronan as a drug delivery system |
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| Authors: | Sorbi Claudia Bergamin Massimo Bosi Susanna Dinon Francesca Aroulmoji Vincent Khan Riaz Murano Erminio Norbedo Stefano |
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| Affiliation: | a Eurand S.p.A., Area Science Park, Padriciano 99, 34012 Trieste, Italy
b Protos Research Institute, Via Flavia 23/1, c/o Sviluppo Italia, 34147 Trieste, Italy |
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| Abstract: | Selective halogenation of hyaluronan and partial halogen substitution by methotrexate led to 6-chloro-6-deoxy-6-O-methotrexylhyaluronan, a potential antitumor drug. The remaining halogen could be further substituted by a second organic carboxylate, leading to mixed esters. 6-O-Acetyl-6-O-methotrexylhyaluronan and 6-O-butyryl-6-O-methotrexylhyaluronan were thus synthesized and characterized by NMR spectroscopy. |
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| Keywords: | Hyaluronan conjugate Methotrexate Drug delivery system |
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