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.
Publication types
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Research Support, Non-U.S. Gov't
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Adenosine Deaminase Inhibitors*
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Antineoplastic Agents / pharmacology*
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Cell Division / drug effects
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Deoxyadenosines / pharmacology
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Kinetics
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Pentostatin / pharmacology
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Purine Nucleosides / pharmacology*
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Ribonucleosides / pharmacology*
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Structure-Activity Relationship
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T-Lymphocytes / cytology
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T-Lymphocytes / drug effects
Substances
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Adenosine Deaminase Inhibitors
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Antineoplastic Agents
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Deoxyadenosines
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Purine Nucleosides
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Ribonucleosides
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Pentostatin
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nebularine
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2'-deoxyadenosine