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Aromatase is a target of pharmacological interest for the treatment of estrogen-dependent cancers. In an effort to develop new therapies to treat breast cancer, a series of 1-phenethyl-1H-[1,2,4]triazole derivatives (6a-6h) were synthesized and evaluated for their efficacy as aromatase inhibitors. Biological tests suggest that these compounds exhibit mild to moderate inhibitory activity to aromatase.