Garelnabi, EAE, Pletsas, D, Li, L, Kiakos, K, Karodia, N, Hartley, JA, Phillips, Roger and Wheelhouse, RT (2012) A Strategy for Imidazotetrazine Prodrugs with Anti-cancer Activity Independent of MGMT and MMR. ACS Medicinal Chemistry Letters, 3 (12). pp. 965-968. ISSN 1948-5875

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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