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Syntheses and antifolate activity of 5-methyl-5-deaza analogs of aminopterin, methotrexate, folic acid, and N10-methylfolic acid

…, GS McCaleb, JA Montgomery, RL Kisliuk…

文献索引:Piper, J. R.; McCaleb, G. S.; Montgomery, J. A.; Kisliuk, R. L.; Gaumont, Y.; Sirotnak, F. M. Journal of Medicinal Chemistry, 1986 , vol. 29, # 6 p. 1080 - 1087

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被引用次数: 85

摘要

Alkyl Deaza Analogues of Folic Acid Antimetabolites having favorably altered transport characteristics but still possessing tight-binding affinity for DHFR. In studies aimed toward greater understanding of transport properties, Sirotnak et al. have observed differences between tumor and normal proliferative tissue in mediated cellular membrane transport of antifolates and in the intracellular y-polyglutamylation of the agents. These biochemical ...