Carcinogenicity of the Antischistosomal Nitrofuran trans-5-Amino-3-[2-(5-nitro-2-furyl)vinyl]-1,2,4-oxadiazole

• Published in: JNCI : Journal of the National Cancer Institute 1984-07, Vol.73 (1), p.151-160
• Main Authors: Dunsford, Harold A., Keysser, C. Hans, Dolan, Patrick M., Seed, John L., Bueding, Ernest
• Format: Article
• Language: English
• Subjects: 5-Amino-3-((5-nitro-2-furyl)vinyl)-1,2,4-oxadiazole - therapeutic use; 5-Amino-3-((5-nitro-2-furyl)vinyl)-1,2,4-oxadiazole - toxicity; Aging; Animals; Biological and medical sciences; Carcinogens; Dose-Response Relationship, Drug; Drug toxicity and drugs side effects treatment; Female; Male; Medical sciences; Mice; Miscellaneous (drug allergy, mutagens, teratogens...); Neoplasms, Experimental - chemically induced; Neoplasms, Experimental - pathology; Nitrofurans - toxicity; Pharmacology. Drug treatments; Schistosoma mansoni; Schistosomiasis - drug therapy
• ISSN: 0027-8874; 1460-2105; 1460-2105
• DOI: 10.1093/jnci/73.1.151

The antischistosomal and antitrypanosomal drug trans-5-amino-3-[2-(5-nitro-2-furyl)vinyl]-1,2,4-oxadiazole [(SQ18506) CAS: 28754-68-9; (E)-amino-3-(2-(5-nitro-2-furyl)-vinyl)-1,2,4-oxadiazole] was carcinogenic for both male and female CD-1 mice when it was administered either in the diet or by gastric intubation. Dose-dependent increases in tumors of the forestomach and lymphatic tissues were observed in all groups receiving SQ18506 including mice infected with Schistosoma mansoni. The predominant tumor observed was squamous cell carcinoma of the forestomach. The presence or absence of schistosome infection did not appear to alter the incidence or distribution of tumors at comparable doses of SQ18506. The incidence of bladder tumors was positively correlated with the dose in gastric intubation studies and inversely correlated with the dose in dietary studies. The carcinogen N-[4-(5-nitro-2-furyl)-2-thiazolyl]formamide (CAS: 24554-26-5) was fed to male and female CD-1 mice in the diet as a positive control. The predominant tumor observed in these groups was transitional cell carcinoma of the bladder. These data indicate that SQ18506 is unsuitable for use in the treatment of parasitic diseases.