Nucleic acid related compounds. 47. Synthesis and biological activities of pyrimidine and purine 'acyclic' nucleoside analogs
| Autor: | Peter W. Hatfield, Morris J. Robins, Erik De Clercq, Jan Balzarini |
|---|---|
| Rok vydání: | 1984 |
| Předmět: |
Purine
Antimetabolites Antineoplastic Pyrimidine Stereochemistry Guanine Vaccinia virus Kidney Antiviral Agents Vesicular stomatitis Indiana virus Cell Line Mice chemistry.chemical_compound Pyrimidine analogue Drug Discovery Animals Simplexvirus Nucleotide Leukemia L1210 chemistry.chemical_classification Uracil Purine Nucleosides Pyrimidine Nucleosides chemistry Nucleic acid Molecular Medicine Thymidine |
| Zdroj: | Journal of Medicinal Chemistry. 27:1486-1492 |
| ISSN: | 1520-4804 0022-2623 |
| DOI: | 10.1021/jm00377a018 |
| Popis: | Various acyclic, i.e., (2-hydroxyethoxy)methyl and (2-acetoxyethoxy)methyl, analogues of pyrimidine and purine nucleosides have been prepared and evaluated for their antiviral, antimetabolic, and cytotoxic properties. All of the pyrimidine analogues, including (E)-5-(2-bromovinyl)-1-[(2-hydroxyethoxy)methyl]uracil (12) and its O-acetyl derivative (13), were virtually devoid of antiviral, cytotoxic, and antimetabolic activities. However, several of the 8-substituted derivatives of 9-[(2-hydroxyethoxy)methyl]guanine (acyclovir) had higher antiviral specificity in vitro than the parent drug. The 8-methyl-, 8-amino-, 8-bromo-, and 8-iodoacyclovir derivatives have activities worthy of further investigation. |
| Databáze: | OpenAIRE |
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