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

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

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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 - Jan 1 1976

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Nitrofurans
Quinazolines
Sarcoma
Thiophenes
Breast Neoplasms
Incidence
Adenocarcinoma
Morpholinos
Transitional Cell Carcinoma
Human Mammary Glands
Small Intestine
Intestines
Sprague Dawley Rats
Squamous Cell Carcinoma
Breast
Kidney

ASJC Scopus subject areas

  • Oncology
  • Cancer Research

Cite this

Comparative carcinogenicity of 5-nitrothiophenes and 5-nitrofurans in rats. / Cohen, Samuel M.; Ertürk, E.; Bryan, George T.

In: Journal of the National Cancer Institute, Vol. 57, No. 2, 01.01.1976, p. 277-282.

Research output: Contribution to journalArticle

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