Isoflavone derivatives are provided comprising a carboxyalkylene moiety linked via its alkylene chain to the aromatic ring and via its carboxy group to an aminoalkyleneamino residue, which, in turn, is covalently linked to a functional group B. The isoflavone derivatives are preferably derived from biochanin A, genistein, and daidzein, and the functional group B is preferably an amino protecting group. These isoflavone derivatives are useful for treating or preventing diseases or disorders associated with estrogen receptor functioning.