Structure-activity relationships of 1-[(2-hydroxyethoxy) methyl]-6-(phenylthio) thymine analogs: effect of substitutions at the C-6 phenyl ring and at the C-5 position on …

H Tanaka, H Takashima, M Ubasawa…

Index: Tanaka, Hiromichi; Takashima, Hideaki; Ubasawa, Masaru; Sekiya, Kouichi; Nitta, Iasei; et al. Journal of Medicinal Chemistry, 1992 , vol. 35, # 2 p. 337 - 345

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Citation Number: 168

Abstract

The effect of substitution on the pyrimidine moiety of 1-[(2-hydroxyethoxy) methyl]-6- (phenylthio) thymine (HEFT) and 1-[(2-hydroxyethoxy) methyl]-6-(phenylthio)-2-thiothymine (HEPT-S) on anti-HIV-1 activity was investigated by synthesizing a series of 5-methyl-6- (arylthio) and 5-substituted-6-(phenylthio) derivatives. Preparation of the 5-methyl-6- (arylthio) derivatives was carried out based on either LDA lithiation of 1-[[2-(tert- ...