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Lipophilic methotrexate conjugates with glucose-lipoamino acid moieties: synthesis and in vitro antitumor activity |
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| Abstract | To obtain methotrexate (MTX) derivs. with a balanced hydrolipophilic character, we synthesized a series of conjugates in which the drug was linked to lipoamino acid (LAA)-glucose residues (LAAG-MTX). These conjugates displayed increased soly. in polar media compared with the corresponding LAA-MTX conjugates previously described. In vitro biol. testing of LAAG-MTX indicated that the introduction of the sugar moiety decreased the biol. activity of these MTX conjugates. The tetradecyl deriv. 6b, however, was effective in inhibiting the dihydrofolate reductase activity in vitro and showed an inhibitory effect on human lymphoblastoid cell growth. | |||
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| Altri Autori | Sorrenti Valeria Vicari Luisa Claudia Spampinato Di Giacomo Giuseppina Toth Istvan |
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