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Strategy for Imidazotetrazine Prodrugs with Anticancer Activity Independent of MGMT and MMR

Yes / The imidazotetrazine ring is an acid-stable precursor and prodrug of highly reactive alkyl diazonium ions. We have shown that this reactivity can be managed productively in an aqueous system for the generation of aziridinium ions with 96% efficiency. The new compounds are potent DNA alkylators and have antitumor activity independent of the O6-methylguanine-DNA methyltransferase and DNA mismatch repair constraints that limit the use of Temozolomide.

Identiferoai:union.ndltd.org:BRADFORD/oai:bradscholars.brad.ac.uk:10454/7241
Date2012 September 1918
CreatorsGarelnabi, Elrashied A.E., Pletsas, Dimitrios, Li, Li, Kiakos, K., Karodia, Nazira, Hartley, J.A., Phillips, Roger M., Wheelhouse, Richard T.
Source SetsBradford Scholars
LanguageEnglish
Detected LanguageEnglish
TypeArticle, Accepted manuscript
Rights(c) 2012 American Chemical Society. Full-text reproduced in accordance with the publisher's self-archiving policy., Unspecified

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