Nucleic acids. 16. Orally active derivatives of ara-cytidine

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Abstract
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, make water soluble by use of their hydrochloride salts or peptidyl derivatives, and 2 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.