Structure-Activity Relationships of Estrogen Derivatives as Aromatase Inhibitors. Effects of Heterocyclic Substituents
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概要
- 論文の詳細を見る
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 (K_i, 2.1±0.14 and 1.53±0.08μM 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.
- 公益社団法人日本薬学会の論文
- 2008-09-01
著者
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NUMAZAWA Mitsuteru
Tohoku College of Pharmacy
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Yamashita Kouwa
Tohoku Pharmaceutical University
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KOMATSU Sachiko
Tohoku Pharmaceutical University
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TOMINAGA Takako
Tohoku Pharmaceutical University
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