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Nearly 300 natural product compounds have been evaluated for their ability to inhibit aromatase, in noncellular, cell-based, and in vivo aromatase inhibition assays. Flavonoids have been tested most frequently and generally found to be the most active class of natural product AI compounds. Some of the more active flavonoids included apigenin ( 8 ), chrysin (11), 7-hydroxyflavone (26), isolicoflavonol (27), (2S)-abyssinone II (45), (2S)-2',4'-dihydroxy-2”-(1-hydroxy-1-methylethyl)dihydrofuro[2,3-h]flavanone (49), eriodictyol (50), 8-prenylnaringenin (62), 3'-[γ-hydroxymethyl-(E)-γ-methylallyl]-2,4,2',4'-tetrahydroxychalcone 11'-O-coumarate (75), isoliquiritigenin (77), and rotenone (132). Other very active AI compounds included the xanthone, γ-mangostin (239), the sesquiterpene lactone, 11βH,13-dihydro-10-epi-8-deoxycumambrin (211), and the anthraquinone, benzanthraquinone I (249).