Toxicity and anticancer activity of a new triazine antifolate (NSC 127755).

Abstract

A new triazine folate antagonist, 3-chloro-4-((4-(2-chloro-4-[4,6-diamino-2,2-dimethyl-s-triazin-1(2H)-yl]phenyl)butyl)) benzenesulfonyl fluoride compounded with ethanesulfonic acid (1:1) (NSC 127755), was highly active against four transplantable colon adenocarcinomas (36, 38, 10/A, 12/A) and the Dunning murine ovarian tumor M5076. Treatment schedule studies indicated that a prolonged time of exposure provided optimum antitumor activity for the compound. The combination of NSC 127755 plus 4-amino-1-[5-O-(1-oxohexadecyl)-beta-D-arabinofuranosyl]-2(1H)-pyrimidinone (palmO-ara-C, NSC 135962) was found to have therapeutic synergism against grossly evident colon adenocarcinoma 36.

• Authors: T H Corbett, W R Leopold, D J Dykes, B J Roberts, D P Griswold Jr, F M Schabel Jr
• Journal: Cancer research (Cancer Res) Vol. 42 Issue 5 Pg. 1707-15 (May 1982) ISSN: 0008-5472 [Print] United States
• PMID: 7066891 (Publication Type: Journal Article, Research Support, U.S. Gov't, P.H.S.)

Chemical References

• Acetamides
• Antimetabolites, Antineoplastic
• Folic Acid Antagonists
• Triazines
• NSC 127755
• Vincristine
• dimethylacetamide

Topics

• Acetamides (therapeutic use)
• Adenocarcinoma (drug therapy, pathology)
• Animals
• Antimetabolites, Antineoplastic (therapeutic use, toxicity)
• Colonic Neoplasms (drug therapy, pathology)
• Drug Administration Schedule
• Drug Evaluation, Preclinical
• Drug Synergism
• Female
• Folic Acid Antagonists
• Mice
• Neoplasm Transplantation
• Neoplasms, Experimental (drug therapy, pathology)
• Ovarian Neoplasms (drug therapy, pathology)
• Triazines (therapeutic use, toxicity)
• Vincristine (therapeutic use)