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A theoretical study of the mechanism of the alkylation of guanine by N-nitroso compounds

Thesis/Dissertation ·
OSTI ID:7308869

N-nitroso compounds are potent, organ-specific carcinogens which effect chemical mutations via alkylation of the DNA base guanine. The resulting G:C [yields] A:T transition is believed to be due to anomalous base pairing of O[sup 6]-alkylguanine with thymine during replication. The ultimate metabolite involved in the alkylation reaction has generally been thought to be an alkyldiazonium ion or its decomposition product, a carbocation. In this study, semiempirical (MOPAC) analysis of the enthalpy changes associated with the alkylation on guanine of the O[sup 6] oxygen, the purported promutagenic site, and the N[sup 7] nitrogen by alkyldiazonium ions and by carbocations indicate that the alkyldiazonium ion is the more likely ultimate mutagen. However, the deprotonation of the N[sup 1] nitrogen, as observed in x-ray studies of O[sup 6]-methylguanine, was not apparent in these semiempirical calculations. Subsequent calculations on the possible involvement of water in the loss of the N[sup 1] hydrogen were performed using both semiempirical and density-functional (DGauss) techniques. The density-functional calculations proved comparable to high-level traditional ab inito calculations on model reactions and allowed such rigor to be reasonably applied to a guanine-sized system. A two-step mechanism is proposed in which an intact alkydiazonium ion attacks the O[sup 6] position and, then, deprotonation at N[sup 1] occurs with water acting as a proton acceptor.

Research Organization:
North Carolina Univ., Chapel Hill, NC (United States)
OSTI ID:
7308869
Country of Publication:
United States
Language:
English