Folate analogs. 32. Synthesis and biological evaluation of 2-desamino-2-methyl-N10-propargyl-5, 8-dideazafolic acid and related compounds

…, F Maley, RL Kisliuk, Y Gaumont, D Duch…

Index: Patil; Jones; Nair; Galivan; Maley; Kisliuk; Gaumont; Duch; Ferone Journal of Medicinal Chemistry, 1989 , vol. 32, # 6 p. 1284 - 1289

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Citation Number: 31

Abstract

The chemical synthesis of three close analogues (2-4) of N'o-propargyl-5, 8-dideazafolate (PDDF) is described. The quinazoline ring of 2 and 4 was constructed from the pivotal intermediate 9 in a novel and unambiguous manner during the final step of the synthesis under very mild conditions. 2-Desamino-2-methyl-N'o-propargyl-5, &dideazafolate (DMPDDF)(2) was a strong inhibitor of human and Lactobacillus casei thymidylate ...