Estradiol conjugated compounds that can target estrogen receptor positive cells and produce lethal N3-methyladenine adducts in these cells have been synthesized and investigated. Prior studies with these DNA methylating compounds had shown that the ability of these molecules to produce N3-methyladenine adducts was crucially dependent on the composition of the linker unit connecting the DNA methylating moiety to the estradiol unit. The DNA binding properties of this class of molecules was investigated using stable non-methylating analogs, and the variation in the DNA binding ability of the compounds was compared to the corresponding DNA methylating ability. Cell toxicity studies were conducted using MCF-7 breast cancer cells in order to determine any correlation between toxicity and DNA methylation and estrogen receptor binding. The results of these studies will be presented.

DNA binding, DNA methylation and cell toxicity of estradiol conjugated DNA methylating compounds

247th National Meeting (2014)

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