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

J Med Chem. 1983 Apr;26(4):544-8. doi: 10.1021/jm00358a016.

Abstract

Several new 3'-azido and 3'-amino nucleosides (8, 9, 12, and 13) have been synthesized and their biological activities evaluated. Among them, 3'-amino-2',3'-dideoxycytidine (13) was found to exhibit potent cytotoxic activity against both L1210 and S-180 cells in vitro with an ID50 of 0.7 and 4.0 microM, respectively. Furthermore, 13 has also shown antitumor activity against L1210 tumor bearing mice with a T/C X 100 value of 283.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Animals
  • Antineoplastic Agents / pharmacology*
  • Body Weight / drug effects
  • DNA Replication / drug effects
  • Leukemia L1210 / metabolism
  • Mice
  • Pyrimidine Nucleosides / chemical synthesis*
  • Pyrimidine Nucleosides / pharmacology

Substances

  • Antineoplastic Agents
  • Pyrimidine Nucleosides