New folate analogs of the 10-deaza-aminopterin series: markedly increased antitumor activity of the 10-ethyl analog compared to the parent compound and methotrexate against some human tumor xenografts in nude mice

Cancer Treat Rep. 1985 May;69(5):551-3.


In an extension of our prior studies in murine tumor models, we examined two new folate analogs in the 10-deaza-aminopterin series for antitumor activity against a group of human tumor xenografts in nude mice. In all three xenograft models studied, MX-1 mammary carcinoma, LX-1 lung carcinoma, and CX-1 colon carcinoma, 10-deaza-aminopterin was minimally active, while methotrexate was inactive. In contrast, against the MX-1 and LX-1 tumors, 10-ethyl, 10-deaza-aminopterin at or near the LD10 dose (2-4.5 mg/kg) given once per day X 5 produced frank regressions. Activity of this analog against the CX-1 tumor was less, but retardation of tumor growth was observed with some minor regressions.

Publication types

  • Comparative Study
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Aminopterin / analogs & derivatives*
  • Aminopterin / therapeutic use
  • Animals
  • Antineoplastic Agents / therapeutic use*
  • Female
  • Folic Acid Antagonists / therapeutic use*
  • Humans
  • Methotrexate / therapeutic use*
  • Mice
  • Mice, Nude
  • Neoplasm Transplantation
  • Neoplasms, Experimental / drug therapy*
  • Transplantation, Heterologous


  • Antineoplastic Agents
  • Folic Acid Antagonists
  • Aminopterin
  • 10-deazaaminopterin
  • Methotrexate