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As part of the safety assessment of (3-[3-(6-benzoyloxy-3-cyano-2- pyridyloxycarbonyl)benzoyl]-1-ethoxymethyl-5-fluorouracil) (BOF-A2), a new 5-fluorouracil (5-FU) derivative with anti-tumour activity, its potential genotoxicity was studied in 3 different tests. BOF-A2 was negative in a reverse mutation (Ames) test in strains of S. typhimurium and E. coli. BOF-A2 induced chromosomal aberrations in Chinese hamster cells in vitro especially in the presence of exogenous metabolic activation, and was clastogenic in vivo, inducing micronuclei in mouse bone marrow. The clastogenic activity of BOF-A2 was similar to that of 5-FU.

journal of toxicological sciences

MUTAGENIC AND CLASTOGENIC PROPERTIES OF (3-[3-(6-BENZOYLOXY-3-CYANO-2-PYRIDYLOXYCARBONYL)BENZOYL]-1-ETHOXYMETHYL-5-FLUOROURACIL)(BOF-A2), A NEW 5-FLUOROURACIL DERIVATIVE WITH ANTI-TUMOUR ACTIVITY