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Garelnabi, EAE; Pletsas, D; Li, L; Kiakos, K; Karodia, N; Hartley, JA; Phillips, Roger; Wheelhouse, RT (2012)
Publisher: ACS Publications
Languages: English
Types: Article
Subjects: RM
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.
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