Lipophilic methotrexate conjugates with antitumor activity

…, V Sorrenti, C Di Giacomo, L Vicari, JJ McGuire…

Index: Pignatello, Rosario; Spampinato, Giuseppina; Sorrenti, Valeria; Di Giacomo, Claudia; Vicari, Luisa; McGuire, John J.; Russell, Cynthia A.; Puglisi, Giovanni; Toth, Istvan European Journal of Pharmaceutical Sciences, 2000 , vol. 10, # 3 p. 237 - 245

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Citation Number: 43

Abstract

Lipophilic methotrexate (MTX)–lipoamino acid conjugates coupled with amide or ester linkages (1a–1r) were synthesised. The inhibitory activity of the conjugates was evaluated on bovine liver DHFR. The in vitro growth inhibitory effect against MTX-sensitive human lymphoblastoid CCRF-CEM cells and an MTX-resistant sub-line (CEM/MTX), which displays defective intracellular transport of MTX, was determined under short-term and continuous ( ...