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• W2014235764 startingPage "1304" @default.
• W2014235764 abstract "Aromatase, which is responsible for the conversion of androgens to estrogens, is a potential therapeutic target for the selective lowering estrogen level in patients with estrogen-dependent breast cancer. We prepared and tested series of the pyridine- and other heterocyclic ring-containing derivatives of 2- and 4-aminoestrones, estrone, and estradiol, compounds 5, 10, 12 and 15. The isonicotinyl derivatives of 2- and 4-aminoestrone, compounds 5c and 10c, were fairly potent competitive inhibitors of aromatase (Ki, 2.1±0.14 and 1.53±0.08 μM for 5c and 10c, respectively) and other compounds did not show, to a significant extent, the aromatase inhibitory activity. This result suggests that the isonicotinyl-substituted derivatives 5c and 10c would be accessible to the active site of aromatase." @default.
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• W2014235764 date "2008-01-01" @default.
• W2014235764 modified "2023-10-16" @default.
• W2014235764 title "Structure-Activity Relationships of Estrogen Derivatives as Aromatase Inhibitors. Effects of Heterocyclic Substituents" @default.
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• W2014235764 doi "https://doi.org/10.1248/cpb.56.1304" @default.
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