Abstract
Aromatase, a cytochrome P450 enzyme complex present in breast tissues, plays a significant role in the biosynthesis of important endogenous estrogens from androgens. The source of estrogen production in breast cancer tissues is intra-tumoral aromatase, and inhibition of aromatase may inhibit the growth stimulation effect of estrogens in breast cancer tissues. Consequently, aromatase is considered a useful therapeutic target in the treatment and prevention of estrogen-dependent breast cancer. Recently, different natural products and synthetic compounds have been rapidly developed, studied, and evaluated for aromatase inhibitory activity. Aromatase inhibitors are classified into two categories on the basis of their chemical structures, i.e., steroidal and nonsteroidal aromatase inhibitors. This review highlights the synthetic steroidal and nonsteroidal aromatase inhibitors reported in the literature in the last few years and will aid medicinal chemists in the design and synthesis of novel and pharmacologically-potent aromatase inhibitors for the treatment of breast cancer.
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•Aromatase inhibitors are competitive inhibitors of the enzyme aromatase, involved in the biosynthesis of estrogen from androgen.•The recent development of steroidal and nonsteroidal aromatase inhibitors was reviewed.•This review provides a pharmacological profile of the most active compound of the corresponding series of derivatives.•Molecular structures and structure activity relationships have been discussed.•The review will be useful for development of novel aromatase inhibitors.