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

Description

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.

Links & Downloads

1. 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.
2. http://hdl.handle.net/10454/7241
3. https://doi.org/10.1021/ml300132t

Tags

Additional Fields

Identifer	oai:union.ndltd.org:BRADFORD/oai:bradscholars.brad.ac.uk:10454/7241
Date	18 September 2012
Creators	Garelnabi, Elrashied A.E., Pletsas, Dimitrios, Li, Li, Kiakos, K., Karodia, Nazira, Hartley, J.A., Phillips, Roger M., Wheelhouse, Richard T.
Source Sets	Bradford Scholars
Language	English
Detected Language	English
Type	Article, Accepted Manuscript
Rights	(c) 2012 American Chemical Society. Full-text reproduced in accordance with the publisher's self-archiving policy.