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• W2151690949 abstract "Human cytochrome P450 aromatase catalyzes with high specificity the synthesis of estrogens from androgens. Aromatase inhibitors (AIs) such as exemestane, 6-methylideneandrosta-1,4-diene-3,17-dione, are preeminent drugs for the treatment of estrogen-dependent breast cancer. The crystal structure of human placental aromatase has shown an androgen-specific active site. By utilization of the structural data, novel C6-substituted androsta-1,4-diene-3,17-dione inhibitors have been designed. Several of the C6-substituted 2-alkynyloxy compounds inhibit purified placental aromatase with IC(50) values in the nanomolar range. Antiproliferation studies in a MCF-7 breast cancer cell line demonstrate that some of these compounds have EC(50) values better than 1 nM, exceeding that for exemestane. X-ray structures of aromatase complexes of two potent compounds reveal that, per their design, the novel side groups protrude into the opening to the access channel unoccupied in the enzyme-substrate/exemestane complexes. The observed structure-activity relationship is borne out by the X-ray data. Structure-guided design permits utilization of the aromatase-specific interactions for the development of next generation AIs." @default.
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• W2151690949 date "2012-09-24" @default.
• W2151690949 modified "2023-09-29" @default.
• W2151690949 title "Novel Aromatase Inhibitors by Structure-Guided Design" @default.
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• W2151690949 doi "https://doi.org/10.1021/jm300930n" @default.
• W2151690949 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/3469775" @default.
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• W2151690949 hasPublicationYear "2012" @default.
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