Abstract
Various 2-halogen-substituted analogues (38, 39, 43 and 44), 3-halogen-substituted analogues (51 and 52), and 2',3'-dihalogen-substituted analogues (57-60) of 3-deazaadenosine and 3-halogen-substituted analogues (61 and 62) of 3-deazaguanosine have been synthesized as potential anticancer and/or antiviral agents. Among these compounds, 3-deaza-3-bromoguanosine (62) showed significant cytotoxicity against L1210, P388, CCRF-CEM and B16F10 cell lines in vitro, producing IC50 values of 3, 7, 9 and 7 microM, respectively. Several 3-deazaadenosine analogues (38, 51, 57 and 59) showed moderate to weak activity against hepatitis B virus.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / pharmacology*
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Antiviral Agents / chemistry*
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Antiviral Agents / pharmacology*
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Biochemistry / methods
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Drug Screening Assays, Antitumor
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Guanosine / analogs & derivatives*
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Guanosine / chemical synthesis*
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Guanosine / chemistry
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Guanosine / pharmacology*
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HIV-1 / drug effects
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Halogens / chemistry
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Hepatitis B virus / drug effects
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Humans
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Inhibitory Concentration 50
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Leukemia L1210
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Microbial Sensitivity Tests
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Tumor Cells, Cultured
Substances
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3-deaza-3-bromoguanosine
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Antineoplastic Agents
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Antiviral Agents
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Halogens
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Guanosine
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3-deazaguanosine