Strategy for Imidazotetrazine Prodrugs with Anticancer Activity Independent of MGMT and MMR
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Publication date
18/09/2012Author
Garelnabi, Elrashied A.E.Pletsas, Dimitrios
Li, Li
Kiakos, K.
Karodia, Nazira
Hartley, J.A.
Phillips, Roger M.
Wheelhouse, Richard T.
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(c) 2012 American Chemical Society. Full-text reproduced in accordance with the publisher's self-archiving policy.Peer-Reviewed
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openAccess
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Show full item recordAbstract
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.Version
Accepted manuscriptCitation
Garelnabi EAE, Pletsas D, Li L, Kiakos K, Karodia N, Hartley JA, Phillips RM and Wheelhouse RT (2012) Strategy for Imidazotetrazine Prodrugs with Anticancer Activity Independent of MGMT and MMR. ACS Medicinal Chemistry Letters. 3(12): 965-968.Link to Version of Record
https://doi.org/10.1021/ml300132tType
Articleae974a485f413a2113503eed53cd6c53
https://doi.org/10.1021/ml300132t