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N⁴-Behenoyl-1-ß-D-arabinofuranosylcytosine as a Potential New Antitumor Agent¹

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

N⁴-Acyl-1-ß-D-arabinofuranosylcytosines, which are lipophilic antitumor analogs of 1-ß-D-arabinofuranosylcytosine, were dissolved by the use of a detergent, HCO-60, and the differences in the antitumor activities when the drugs were administered in the forms of solution or suspension were compared. N⁴-Stearoyl-1-ß-D-arabinofuranosylcytosine (NSC 201290), which was the most active compound when administered as an aqueous suspension, diminished in its activities after it had been dissolved into a clear solution, whereas N⁴-behenoyl-1-ß-D-arabinofuranosylcytosine (NSC 239336) exhibited activities superior to those of the parent compound 1-ß-D-arabinofuranosylcytosine when administered as a solution. Moreover, the high efficacy of this compound was long lasting in the host animal, regardless of the treatment schedules or the presence of the 1-ß-D-arabinofuranosylcytosine-inactivating enzyme, cytidine deaminase.

¹ This experiment was supported by part by a Grant-in-Aid for cancer research from the Ministry of Education, Science, and Culture, and the Ministry of Health and Welfare, Tokyo, Japan.

Received 1/24/77. Accepted 4/28/77.