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Antitumor Activities of Newly Synthesized N⁴-Acyl-1-ß-D-arabinofuranosylcytosine¹

Division of Experimental Chemotherapy, Cancer Chemotherapy Center, Japanese Foundation for Cancer Research, Kami-Ikebukuro 1-37-1, Toshima-ku, Tokyo, 170, Japan [M. A., S. T., S. A.], and Technical Research Laboratory, Asahi Chemical Industry Co., Ltd., Samejima 2-1, Fuji, Shizuoka, 416, Japan [J. O., T. I., H. K.]

New derivatives of 1-ß-D-arabinofuranosylcytosine were synthesized and their antitumor activities were tested against mouse leukemia L1210. Among the 50 compounds investigated, a series of N⁴-acyl derivatives with long-chain saturated fatty acids were found to be highly active. The most active derivatives were N⁴-stearoyl-1-ß-D-arabinofuranosylcytosine, which was administered in the form of suspension, and N⁴-behenoyl-1-ß-D-arabinofuranosylcytosine given in the form of solution. They were superior to the parent compound, 1-ß-D-arabinofuranosylcytosine, in that smaller dosages exhibited strong activities regardless of the treatment schedule, and they were also resistant to cytidine deaminase.

¹ This experiment was supported in part by a Grant-in-Aid for Cancer Research from the Ministry of Education, Science and Culture, Japan.

² To whom requests for reprints should be sent.

Received 2/ 2/76. Accepted 4/13/76.

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