کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1378247 | 981997 | 2007 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Synthesis and identification of novel oxa-steroids as progesterone receptor antagonists
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Synthesis and identification of novel oxa-steroids as progesterone receptor antagonists Synthesis and identification of novel oxa-steroids as progesterone receptor antagonists](/preview/png/1378247.png)
چکیده انگلیسی
A novel series of oxa-steroids 6 derived from (8S, 13S, 14R)-7-oxa-estra-4,9-diene-3,17-dione 1 have been synthesized and identified as potent and selective progesterone receptor antagonists. These novel oxa-steroids showed similar potency to mifepristone. Preliminary SAR study resulted in the most potent 17-phenylethynyl oxa-steroid 6i wih an IC50 of 1.4 nM. In contrast to the equipotent mifepristone toward the progesterone receptor (PR) and glucocorticoid receptor (GR), compound 6i had over 200-fold selectivity for PR over GR.
Novel 7-oxa-steroids were synthesized and indentified as new potent and selective progesterone receptor antagonists.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 17, Issue 4, 15 February 2007, Pages 907–910
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 17, Issue 4, 15 February 2007, Pages 907–910
نویسندگان
Fu-An Kang, George Allan, Jihua Guan, Nareshkumar Jain, Olivia Linton, Pamela Tannenbaum, Jun Xu, Peifang Zhu, Joseph Gunnet, Xin Chen, Keith Demarest, Scott Lundeen, Zhihua Sui,