Synthesis and antineoplastic activity of 3'-azido and 3'-amino analogs of pyrimidine deoxyribonucleoside

Abstract
Several new 3''-azido and 3''-amino nucleosides (8, 9, 12 and 13) were synthesized and their biological activities evaluated. Among them, 3''-amino-2'',3''-dideoxycytidine (13) was found to exhibit potent cytotoxic activity against both L1210 [murine leukemia] and S-180 [murine sarcoma] cells in vitro with an ID50 [median inhibitory dose] of 0.7 and 4.0 .mu.M, respectively. Furthermore, 13 has also shown antitumor activity against L1210 tumor bearing mice with a T/C .times. 100 value of 283.