title: Nonsteroidal aromatase inhibitors for the treatment of breast cancer: an update.
abstract: 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.
authors.forename: Silvia
authors.initials: S
authors.lastname: Gobbi
authors.forename: Angela
authors.initials: A
authors.lastname: Rampa
authors.forename: Federica
authors.initials: F
authors.lastname: Belluti
authors.affiliation: Department of Pharmaceutical Sciences, University of Bologna, Via Belmeloro, 6, I-40126 Bologna, Italy. silvia.gobbi@unibo.it.
authors.forename: Alessandra
authors.initials: A
authors.lastname: Bisi
mesh_terms: D016588:Anticarcinogenic Agents / Q000737:chemistry / Q000627:therapeutic use; D000970:Antineoplastic Agents / Q000737:chemistry / Q000627:therapeutic use*; D001141:Aromatase / Q000235:genetics / Q000378:metabolism; D047072:Aromatase Inhibitors / Q000737:chemistry / Q000627:therapeutic use*; D001943:Breast Neoplasms / Q000188:drug therapy* / Q000201:enzymology / Q000517:prevention & control; D015195:Drug Design; D019008:Drug Resistance, Neoplasm; D020847:Estrogen Receptor Modulators / Q000627:therapeutic use; D005260:Female; D005419:Flavonoids / Q000737:chemistry / Q000627:therapeutic use; D006801:Humans; D043266:Steryl-Sulfatase / Q000037:antagonists & inhibitors / Q000378:metabolism; D013329:Structure-Activity Relationship; D013629:Tamoxifen / Q000627:therapeutic use
chemical_list: D016588:Anticarcinogenic Agents; D000970:Antineoplastic Agents; D047072:Aromatase Inhibitors; D020847:Estrogen Receptor Modulators; D005419:Flavonoids; D013629:Tamoxifen; D001141:Aromatase; D043266:Steryl-Sulfatase