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

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 D...

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Bibliographic Details
Published in:Cancer research (Chicago, Ill.) Ill.), 1982-05, Vol.42 (5), p.1707
Main Authors: Corbett, T H, Leopold, W R, Dykes, D J, Roberts, B J, Griswold, Jr, D P, Schabel, Jr, F M
Format: Article
Language:English
Subjects:
Acetamides - therapeutic use
Adenocarcinoma - drug therapy
Adenocarcinoma - pathology
Animals
Antimetabolites, Antineoplastic - therapeutic use
Antimetabolites, Antineoplastic - toxicity
Colonic Neoplasms - drug therapy
Colonic Neoplasms - pathology
Drug Administration Schedule
Drug Evaluation, Preclinical
Drug Synergism
Female
Folic Acid Antagonists
Mice
Neoplasm Transplantation
Neoplasms, Experimental - drug therapy
Neoplasms, Experimental - pathology
Ovarian Neoplasms - drug therapy
Ovarian Neoplasms - pathology
Triazines - therapeutic use
Triazines - toxicity
Vincristine - therapeutic use
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Summary: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.
ISSN:0008-5472