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

Samuel M. Cohen, E. Ertürk, George T. Bryan

Research output: Contribution to journalArticle

12 Scopus citations

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).

Original languageEnglish (US)
Pages (from-to)277-282
Number of pages6
JournalJournal of the National Cancer Institute
Volume57
Issue number2
DOIs
StatePublished - 1976

ASJC Scopus subject areas

  • Oncology
  • Cancer Research

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