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)-β-d-arabinofuranosyl]-2(1H)-pyrimidinone (palmO-ara-C, NSC 135962) was found to have therapeutic synergism against grossly evident colon adenocarcinoma 36.

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The work reported herein was supported by Contract NO1-CM-97309 with the Division of Cancer Treatment, National Cancer Institute, NIH, Department of Health and Human Services; by Grant CA 17303 from the National Large Bowel Cancer Project, the University of Texas System Cancer Center, M. D. Anderson Hospital and Tumor Institute; and by grant RO1-CA-26485 from the National Cancer Institute, NIH, Department of Health and Human Services.

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