10-Propargylaminopterin and alkyl homologs of methotrexate as inhibitors of folate metabolism

…, 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, 1982 , vol. 25, # 7 p. 877 - 880

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被引用次数: 25

摘要

Reported antifolate activity against leukemia L1210 by N-[4-[[(2-amino-4-hydroxy-6- quinazolinyl) methyl]-propargylamino] benzoyl]-glutamic acid through potent inhibition of thymidylate synthase (EC 2.1. 1.45) prompted us to include the propargyl group in a study of the effect on folate metabolism and membrane transport of replacing the 10-methyl group of methotrexate with other groups. Along with the propyl (8a) and octyl (8b) homologues of ...