Estrogens are known to be important in breast cancer growth in both pre- and post-menopausal women. Although circulating
estrogen concentrations are very low after menopause, peripheral tissues generate sufficient concentrations to stimulate tumor growth. As
aromatase is the rate-limiting enzyme in estrogen biosynthesis, inhibitors of this enzyme represent effective targeted therapy for breast
cancer. Three compounds are now FDA approved and have become the first-choice endocrine drugs for postmenopausal breast cancer
patients, since they are associated with superior activity and better general tolerability when compared with the estrogen receptor
modulator tamoxifen. Nevertheless, some questions concerning the use of aromatase inhibitors for the treatment of breast cancer still
need to be addressed, mainly related to their side-effects and the development of resistance, making research in this field still appealing.
Many research groups, including our own, are still dealing with the search of new compounds that possess aromatase inhibitory
properties. In this review an update of the latest achievements in the field of nonsteroidal aromatase inhibitors will be given.
Keywords: Anticancer, aromatase inhibitors, breast cancer, chemopreventive, cytochrome P450, CYP19, drug discovery, endocrine therapy,
estrogens, flavonoids, natural products, nonsteroidal.
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