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…

Index: 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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Citation Number: 85

Abstract

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 ...