Journal of medicinal chemistry

Methotrexate analogs. 19. Enhancement of the antitumor effect of methotrexate and 3', 5'-dichloromethotrexate by the use of lipid-soluble diesters

A Rosowsky, CS Yu

Index: Rosowsky, A.; Yu, C.-S. Journal of Medicinal Chemistry, 1983 , vol. 26, # 10 p. 1448 - 1452

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Citation Number: 11

Abstract

Lipophilic methotrexate (MTX) and 3',5'-dichloromethotrexate (DCM) diesters were prepared by HC1-catalyzed esterification or by neutral esterification using cesium carbonate and an alkyl or aralkyl halide in Me2S0. The products were tested for in vivo antitumor activity against L1210 leukemia in mice to test whether all MTX and DCM diesters are therapeutically equivalent in this species. Contrary to what has been found with simple primary dialkyl esters, ortho- ...