Inhibition of adenosine deaminase by azapurine ribonucleosides.
作者信息
Shewach D S, Krawczyk S H, Acevedo O L, Townsend L B
机构信息
Department of Pharmacology, University of Michigan Medical School, Ann Arbor 48109.
出版信息
Biochem Pharmacol. 1992 Nov 3;44(9):1697-700. doi: 10.1016/0006-2952(92)90061-m.
PMID:1449528
Abstract
We have synthesized several 8-azapurine nucleosides as inhibitors of adenosine deaminase. The presence of a nitrogen on the imidazole ring decreased the Ki value for nebularine by 100-fold but did not lower the Ki value for coformycin. Evaluation of these compounds in a MOLT-4 growth assay revealed that 2-azacoformycin was as effective as 2'-deoxycoformycin in potentiating growth inhibition by 2'-deoxyadenosine. The azapurine nucleosides merit further study as antitumor agents.
摘要
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