Nucleosides of azathioprine and thiamiprine as antiarthritics

TA Krenitsky, WW Hall, JL Selph, JF Truax…

Index: Krenitsky, Thomas A.; Hall, Willard W.; Selph, Jeffrey L.; Truax, James F.; Vinegar, Ralph Journal of Medicinal Chemistry, 1989 , vol. 32, # 7 p. 1471 - 1475

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Citation Number: 11

Abstract

Azathioprine [Imuran; 6-[(l-methyl-4-nitro-1H-imidazol-5-yl) thio]-1H-purine] is a widely used immunosuppressive and antiarthritic drug. For the sake of comparison, the riboside, the 2 '- deoxyriboside, and the arabinoside of azathioprine and its 2-amino congener, thiamiprine, were prepared by an enzymatic method. In vitro, the cytotoxicities of these aglycons and their nucleosides were similar (EDSo= 0.8-2 pM), except for the arabinosides, which were ...