Nucleic acids. 16. Orally active derivatives of ara-cytidine
| Autor: | D. T. Gish, R. L. Griffin, A. J. Gibbons, L. G. Gray, Margaret E. Greig, G. L. Neil, G. D. Gray, S. L. Kuentzel, T. E. Moxley, William J. Wechter |
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| Rok vydání: | 1976 |
| Předmět: |
Encephalomyelitis
Autoimmune Experimental Hydrochloride Anti-Inflammatory Agents Administration Oral Pharmacology Mice chemistry.chemical_compound Oral administration Drug Discovery medicine Animals Leukemia L1210 Antitumor activity Cytarabine Nucleic acid methods food and beverages Cytidine biochemical phenomena metabolism and nutrition Rats carbohydrates (lipids) Orally active chemistry Nucleic acid Molecular Medicine Immunosuppressive Agents medicine.drug |
| Zdroj: | Journal of Medicinal Chemistry. 19:1013-1017 |
| ISSN: | 1520-4804 0022-2623 |
| DOI: | 10.1021/jm00230a007 |
| Popis: | Water-soluble derivatives of ara-cytidine (cytarabine, Cytosar) were prepared and tested for antitumor, immunosuppressive, and antiarthritic activities in animals after oral administration. The compounds tested included the 5'-palmitate, 5'-benzoate, and 5'-adamantoate esters of ara-cytidine, made water soluble by use of their hydrochloride salts of peptidyl derivatives, and two basic 5' esters (5'-nicotinoate and 5'-quinuclidinate) as their hydrochloride salts. Five of the compounds had antitumor activity superior to that found with ara-cytidine itself after oral administration in the L1210 leukemic mouse assay. One of these, 5'-adamantoyl-ara-cytidine hydrochloride, had antitumor activity after oral administration approaching that achieved with parenterally administered ara-cytidine. |
| Databáze: | OpenAIRE |
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