Synthesis of 7- and 10-spermine conjugates of paclitaxel and 10-deacetyl-paclitaxel as potential prodrugs |
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Authors: | Arturo Battaglia Andrea Guerrini Greta Varchi Ezio Bombardelli |
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Affiliation: | a Istituto CNR per la Sintesi Organica e Fotoreattività ‘I.S.O.F.’, Area della Ricerca di Bologna, via P. Gobetti 101, 40129 Bologna, Italy b Indena SPA, viale Ortles 12, 20139 Milano, Italy |
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Abstract: | Efficient syntheses of two taxol analogs bearing the linear polyamine spermine at 7- and 10-positions of paclitaxel and 10-deacetyl-paclitaxel have been developed. These polyamine-taxol-conjugates were isolated as water soluble difluoride salts. The aim of the present work was to introduce a chemical modification into taxol skeleton in order to increase drug selectivity toward tumor cells. The cytotoxic activity of these conjugates was evaluated in MCF7 and MCF7-R cell lines. The observed low cytotoxicity suggests that these conjugates could act as potential prodrugs. |
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Keywords: | Paclitaxel Spermine Prodrug conjugates Antitumor |
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