Folate analogs. 35. Synthesis and biological evaluation of 1-deaza, 3-deaza, and bridge-elongated analogs of N10-propargyl-5, 8-dideazafolic acid

…, RL Kisliuk, Y Gaumont, IK Dev, DS Duch…

Index: Li; Nair; Edwards; Kisliuk; Gaumont; Dev; Duch; Humphreys; Smith; Ferone Journal of Medicinal Chemistry, 1991 , vol. 34, # 9 p. 2746 - 2754

Full Text: HTML

Citation Number: 51

Abstract

Structural modifications at the pyrimidine ring and at the C9, N'O-bridge region of the thymidylate synthase (TS) inhibitors@ o-propargyl-5, sdideezafolate (1; PDDF CB 3717), 2 d~ o-IP o-pr 5,~~ d~ o~ te(2, DPDDF), and 2-desamino-2-methyl-IPo-propargyl-5, 8- dideazafolate (3, DMPDDF) have been carried out. Methods for the synthesis of 2-desamino- @ o-propargyl-1, 5, 8-tridedolate (41, 2-desamino-2-methyl-IPo-propargyl-3, 5, 8- ...