Synthesis and biological activities of tetrahydroquinazoline analogs of aminopterin and methotrexate

A Gangjee, N Zaveri, SF Queener…

Index: Gangjee; Zaveri; Queener; Kisliuk Journal of Heterocyclic Chemistry, 1995 , vol. 32, # 1 p. 243 - 247

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Citation Number: 6

Abstract

Abstract (6R, 6S)-5, 8-Dideaza-5, 6, 7, 8-tetrahydroaminopterin (1) and (6R, 6S)-5, 8- dideaza-5, 6, 7, 8-tetrahydromethotrexate (2) were synthesized as potential inhibitors of dihydrofolate reductase (DHFR) and as antitumor agents. Cyclohexanone-4- carboxaldehyde dimethyl acetal, a key intermediate [10] was synthesized from cyclohexane- 1, 4-dione monoethylene ketal, which was converted via a Wittig reaction to its exocyclic 4 ...