Abstract
Addition of two equivalents of triethyl phosphite to β-arylethylisocyanides to synthesize tetraethyl aminomethylidenebisphosphonates in the presence of a stoichiometric amount of hydrogen chloride is reported. Acid hydrolysis of the tetraethyl esters gave the 2-arylethylaminomethylidenebisphosphonic acids in good yields. Additionally, the obtained bisphosphonates were evaluated for their antiproliferative effect against MCF-7 human breast cancer cells, J774E mouse macrophages and HL-60 human promyelocytic leukemia cells. β-Phenylphenethylamine derivative showed a selective activity towards J774E cells with IC50 values three times lower than Incadronate and twice as high as Zoledronate.
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