Folate analogs. 30. Synthesis and biological evaluation of N10-propargyl-5, 8-dideaza-5, 6, 7, 8-tetrahydrofolic acid and related compounds.

…, R Dhawan, M Ghazala, TI Kalman…

Index: Nair; Dhawan; Ghazala; Kalman; Ferone; Gaumont; Kisliuk Journal of Medicinal Chemistry, 1987 , vol. 30, # 7 p. 1256 - 1261

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Citation Number: 10

Abstract

The 5, 6, 7&tetrahydro derivative (I) of the powerful thymidylate synthase inhibitor~ 0- propargyl-5, 8-dideazafolic acid (PDDF) has been synthesized and evaluated for its antifolate activity. A convenient method for the preparation of the key intermediate 2-amino-6- (bromomethyl)-4-hydroxy-5, 6, 7, 8-tetrahydroquinazoline (18) is described. Two closely related analogues of 1 were also synthesized and evaluated for their antifolate activity and ...