Synthesis, antifolate, and antitumor activities of classical and nonclassical 2-amino-4-oxo-5-substituted-pyrrolo [2, 3-d] pyrimidines

…, JJ McGuire, SF Queener, RL Kisliuk

文献索引：Gangjee; Vidwans; Elzein; McGuire; Queener; Kisliuk Journal of Medicinal Chemistry, 2001 , vol. 44, # 12 p. 1993 - 2003

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被引用次数: 76

摘要

Classical and nonclassical isosteric C8-N9 bridged analogues of the multitargeted antifolate LY231514 were synthesized as inhibitors of thymidylate synthase (TS), dihydrofolate reductase (DHFR), and as antitumor and antiopportunistic infection agents. The syntheses of the analogues were accomplished by reductive amination of the appropriate anilines with 2- amino-4-oxo-5-cyanopyrrolo [2, 3-d] pyrimidine (28) followed by saponification of the ethyl ...