Methotrexate analogs. 14. Synthesis of new. gamma.-substituted derivatives as dihydrofolate reductase inhibitors and potential anticancer agents

A Rosowsky, R Forsch, J Uren…

文献索引：Rosowsky, Andre; Forsch, Ronald; Uren, Jack; Wick, Michael Journal of Medicinal Chemistry, 1981 , vol. 24, # 12 p. 1450 - 1455

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被引用次数: 76

摘要

On this basis, a reasonable approach to the design of new MTX analogues with increased antitumor selectivity, a qualitatively modified therapeutic spectrum, or a more prolonged duration of pharmacological action might be to replace the y-COOH group by other functional groups, such as esters or amides. Depending on whether cleavage of the ester or amide bond occurs in vivo, such compounds could either act as antifols by themselves or ...