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 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.
D000081:Acetamides / Q000627:therapeutic use; D000230:Adenocarcinoma / Q000188:drug therapy / Q000473:pathology; D000818:Animals; D000964:Antimetabolites, Antineoplastic / Q000627:therapeutic use* / Q000633:toxicity; D003110:Colonic Neoplasms / Q000188:drug therapy* / Q000473:pathology; D004334:Drug Administration Schedule; D004353:Drug Evaluation, Preclinical; D004357:Drug Synergism; D005260:Female; D005493:Folic Acid Antagonists; D051379:Mice; D009368:Neoplasm Transplantation; D009374:Neoplasms, Experimental / Q000188:drug therapy / Q000473:pathology; D010051:Ovarian Neoplasms / Q000188:drug therapy* / Q000473:pathology; D014227:Triazines / Q000627:therapeutic use* / Q000633:toxicity; D014750:Vincristine / Q000627:therapeutic use
D000081:Acetamides; D000964:Antimetabolites, Antineoplastic; D005493:Folic Acid Antagonists; D014227:Triazines; C031776:NSC 127755; D014750:Vincristine; C013959:dimethylacetamide