| Boronic acids-A novel class of bacterial mutagen. | |
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MedLine Citation:
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PMID: 21645632 Owner: NLM Status: Publisher |
Abstract/OtherAbstract:
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Boronic acids and their esters are important building blocks in organic syntheses including those for drug substances and for which, as far as it can be determined, there are no published reports of testing for genotoxicity. A number of boronic acids have now been tested in this laboratory using Salmonella typhimurium strains TA1535, TA1537, TA98 and TA100 and Escherichia coli strain WP2uvrA(pKM101). Twelve of the 13 structures presented here were found to be mutagenic. All the compounds except one were active only in TA100 and/or WP2uvrA(pKM101), did not require S9 activation and produced relatively weak responses, i.e. no more than seven times the concurrent solvent-control values at >1000μg/plate. The single exception was also weakly mutagenic for TA1537 in the presence of S9. Results with two compounds mutagenic for both TA100 and WP2uvrA(pKM101) showed no evidence of DNA-adduct formation detectable by (32)P-postlabelling. It appears that boronic acids represent a novel class of bacterial mutagen that may not act by direct covalent binding to DNA. However, their mechanism of action remains to be elucidated and it cannot yet be determined whether or not they present a real genotoxic hazard. |
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Authors:
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Michael R O'Donovan; Christine D Mee; Simon Fenner; Andrew Teasdale; David H Phillips |
Publication Detail:
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Type: JOURNAL ARTICLE Date: 2011-5-26 |
Journal Detail:
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Title: Mutation research Volume: - ISSN: 0027-5107 ISO Abbreviation: - Publication Date: 2011 May |
Date Detail:
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Created Date: 2011-6-7 Completed Date: - Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 0400763 Medline TA: Mutat Res Country: - |
Other Details:
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Languages: ENG Pagination: - Citation Subset: - |
Copyright Information:
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Copyright © 2011 Elsevier B.V. All rights reserved. |
Affiliation:
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Astrazeneca R&D, Alderley Park, Macclesfield, SK10 4TG, United Kingdom. |
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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