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• W2007620585 abstract "Searching for a novel family of inactivators of the human DNA repair protein O6-methylguanine-DNA methyltransferase (MGMT) which is known to bind to the DNA minor groove, we have computationally modelled and synthesised two series of 2-amino-6-aryloxy-5-nitropyrimidines with morpholino or aminodiaryl substituents (potential minor groove binders) at the 4-position. Synthesis of these compounds was achieved by successive substitution of each of the two Cl atoms of 2-amino-4,6-dichloro-5-nitropyrimidine by the corresponding amino and aryloxy derivatives. Biochemical evaluation of these compounds as MGMT inactivators showed poor activities, but in general the 4-bromothenyloxy derivatives showed better inactivation than the benzyloxy versions. DNA binding assessment was not possible due to insolubility problems." @default.
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• W2007620585 date "2011-03-01" @default.
• W2007620585 modified "2023-10-16" @default.
• W2007620585 title "Towards more specific O6-methylguanine-DNA methyltransferase (MGMT) inactivators" @default.
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• W2007620585 doi "https://doi.org/10.1016/j.bmc.2011.01.038" @default.
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