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 Journal Article


Authors: Schmid, F. A.; Sirotnak, F. M.; Otter, G. M.; DeGraw, J. I.
Article Title: 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
Abstract: 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.
Keywords: cancer chemotherapy; human cell; dose response; drug efficacy; antineoplastic agents; comparative study; methotrexate; mouse; animal; mice; breast; animal experiment; animal model; tumor xenograft; nude mouse; mice, nude; drug response; neoplasms, experimental; transplantation, heterologous; tumor model; neoplasm transplantation; folic acid antagonists; therapy; aminopterin; 10 deazaaminopterin; respiratory system; drug comparison; large intestine; intraperitoneal drug administration; edatrexate; human; female; priority journal; support, u.s. gov't, p.h.s.; 10 deazaaminopterin derivative; cell strain cx1; cell strain lx1; cell strain mx 1
Journal Title: Cancer Treatment Reports
Volume: 69
Issue: 5
ISSN: 0361-5960
Publisher: National Cancer Institute  
Date Published: 1985-05-01
Start Page: 551
End Page: 553
Language: English
PUBMED: 4005878
PROVIDER: scopus
DOI/URL:
Notes: Article -- Export Date: 26 October 2021 -- Source: Scopus
Citation Impact
MSK Authors
  1. Francis M Sirotnak
    184 Sirotnak
  2. Glenys M. Otter
    27 Otter
  3. Franz A. Schmid
    26 Schmid