Potent enzyme-activated inhibition of aromatase by a 7 alpha-substituted C19 steroid.
نویسندگان
چکیده
منابع مشابه
Synthesis and screening of aromatase inhibitory activity of substituted C19 steroidal 17-oxime analogs.
The synthesis and aromatase inhibitory activity of androst-4-en-, androst-5-en-, 1β,2β-epoxy- and/or androsta-4,6-dien-, 4β,5β-epoxyandrostane-, and 4-substituted androst-4-en-17-oxime derivatives are described. Inhibition activity of synthesized compounds was assessed using aromatase enzyme and [1β-3H]androstenedione as substrate. Most of the compounds displayed similar to or more aromatase in...
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7or-(4'-Amino)phenylthio-l,4-androstadiene-3,17-dione(7a-APTADD), a potent enzyme-activated irreversible inhibitor, was examined in two different human cell culture lines, MCF-7 human mammary carcinoma cells and JAr choriocarcinoma cells. Both the MCF-7 and JAr cell culture systems exhibit aromatase activity, and 7a-APTADD was evaluated for its aromatase-inhibitory activity, for its ability to ...
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7or-(4'-Amino)phenylthio-l,4-androstadiene-3,17-dione(7a-APTADD), a potent enzyme-activated irreversible inhibitor, was examined in two different human cell culture lines, MCF-7 human mammary carcinoma cells and JAr choriocarcinoma cells. Both the MCF-7 and JAr cell culture systems exhibit aromatase activity, and 7a-APTADD was evaluated for its aromatase-inhibitory activity, for its ability to ...
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Steroid glucuronidation by UDP-glucuronosyltransferase (UGT) enzymes is a mechanism leading to catabolism and elimination of steroid hormones. To establish an animal model to investigate the conjugation of steroids by UGT enzymes, previous results revealed that simian and human are unique in having high levels of circulating androsterone glucuronide and androstane-3alpha, 17beta-diol (3d-Diol) ...
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ژورنال
عنوان ژورنال: Journal of Biological Chemistry
سال: 1987
ISSN: 0021-9258
DOI: 10.1016/s0021-9258(18)47468-6