Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 16, Issue 3, Pages 1474-1480Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2007.10.057
Keywords
7,8-benzoflavanones; flavonoids; aromatase inhibitors; breast cancer
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Some natural compounds such as flavonoids are known to possess a moderate inhibitory activity against aromatase, this enzyme being an interesting target for hormone-dependent breast cancer treatment. It has been demonstrated that the modulation of flavonoid skeleton could increase anti-aromatase effect. Therefore, new 7,8-benzoflavanones were synthesized and tested for their activity toward aromatase inhibition. It was observed that the introduction of a benzo ring at position C-7 and C-8 on flavanone skeleton led to new potent aromatase inhibitors, the resulting 7,8-benzoflavanones being until nine times more potent than amino-gluthetimide (the first aromatase inhibitor used clinically). (C) 2007 Elsevier Ltd. All rights reserved.
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