From Nonsteroidal Aromatase Inhibitors to Multifunctional Drug Candidates: Classic and Innovative Strategies for the Treatment of Breast Cancer

Author(s): Silvia Gobbi, Andrea Cavalli, Alessandra Bisi, Maurizio Recanatini

Journal Name: Current Topics in Medicinal Chemistry

Volume 8 , Issue 10 , 2008

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Aromatase is the enzyme responsible for the conversion of androgens to estrogens and represents the main source of local estrogens in post-menopausal breast cancer tissue. Nonsteroidal aromatase inhibitors (NSAIs) are able to reduce growth-stimulatory effects of estrogens in hormone-dependent breast cancer, and third generation NSAIs are currently approved as first-line therapy for the treatment of postmenopausal women with metastatic advanced breast cancer. Nevertheless, some issues in this area still need to be addressed and research efforts are aimed both at identifying new molecules of therapeutic interest and at exploring different options for the modulation of this enzyme. In this review, an update of the latest developments in the field of NSAIs is presented, to provide a broad view on the recent progress in this area. Beside classical structure-activity relationships studies and development of natural product derivatives, rational approaches for both ligand- and structure-based design are described. Moreover, novel strategies for the development of multitarget-directed molecules are also presented. Finally, some possible future developments in this research area are briefly considered.

Keywords: Drug discovery, breast cancer, antiestrogen, CYP-450, structure-activity relationships

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Article Details

Year: 2008
Published on: 01 March, 2012
Page: [869 - 887]
Pages: 19
DOI: 10.2174/156802608784911590
Price: $65

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