Comparative carcinogenicity of 5-nitrothiophenes and 5-nitrofurans in rats

Cohen S. M., Ertürk E., Bryan G. T.

Journal of the National Cancer Institute, vol.57, no.2, pp.277-282, 1976 (SCI-Expanded) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 57 Issue: 2
  • Publication Date: 1976
  • Doi Number: 10.1093/jnci/57.2.277
  • Journal Name: Journal of the National Cancer Institute
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus, Academic Search Premier, PASCAL, Agricultural & Environmental Science Database, BIOSIS, CAB Abstracts, CINAHL, EMBASE, Food Science & Technology Abstracts, Gender Studies Database, International Pharmaceutical Abstracts, MEDLINE, Public Affairs Index, Veterinary Science Database
  • Page Numbers: pp.277-282
  • Ankara University Affiliated: No

Abstract

We investigated the carcinogenicity of five 5-nitrothiophenes with heterocyclic substituents at the 2-position of the thiophene ring by feeding the chemicals to Sprague-Dawley rats and comparing the type and incidence of lesions with those appearing after exposure to two 5-nitrofurans. Benign and malignant mammary tumors and intestinal tract sarcomas were the most frequent lesions induced by 5-nitrothiophenes. 4-Bis(2-hydroxyethyl) amino-2-(5-nitro-2-thienyl)quinazoline caused a 100% incidence of mammary adenocarcinomas in 28 female rats at risk; it induced 3 benign and 5 malignant mammary tumors and 13 small intestine sarcomas in 20 male rats. A high incidence of similar lesions was observed in male and female rats fed the corresponding 5-nitrofuran analogue, 4-bis(2-hydroxyethyl) amino-2-(5-nitro-2-furyl)quinazoline. In marked contrast, 4 of 28 female rats receiving 4-bis(2-hydroxyethyl)amino-2-(2-thienyl) quinazoline, which lacks the nitro group at the 5-position on the thiophene ring, had solitary benign mammary tumors (P ˃; 0.2). Additional 5-nitrothiophenes demonstrating significant oncogenic activity for female rats were 4-morpholino-2-(5-nitro-2-thienyl) quinazoline, 4-(2-hydroxyethylamino)-2-(5-nitro-2-thienyl) quinazoline, 4-(2, 3-dihydroxypropylamino)-2-(5-nitro-2-thienyl) quinazoline, and 1, 2-dihydro-2-(5-nitro-2-thienyl)quinazolin-4(3H)-one. Another nitrofuran, 4, 6-dimethyl-2-(5-nitro-2-furyl)-pyrimidine, provided the following types of neoplasms in 30 female rats at risk: squamous cell carcinomas of the forestomach (30), sarcomas of the intestine (21), adenocarcinomas of the mammary gland (12), and transitional cell carcinomas of the kidney (2). © 1976, Oxford University Press.