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Following syntheses of novel eight bis(\u03b1\u2010aminoalkyl)phosphinic acid derivatives (<jats:bold>4a\u2013h<\/jats:bold>) as a result of array of reactions, compounds were evaluated by cytotoxic effects<jats:italic>in vitro<\/jats:italic>on human breast cancer (MCF\u20107) and normal endothelial (HUVEC) cell lines. All phosphinic acid derivatives were effective for cytotoxicity on both MCF\u20107 and HUVEC lines, while<jats:bold>4c<\/jats:bold>,<jats:bold>4e<\/jats:bold>, and<jats:bold>4f<\/jats:bold>compounds were found significantly more effective. For the evaluation of antitumor properties of compounds in a highly sensitive method, their effects on inhibiting topoisomerases I and II were investigated. 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