کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1376768 | 981964 | 2006 | 6 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Newly discovered orally active pure antiestrogens
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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چکیده انگلیسی
In order to develop orally active pure antiestrogens, we incorporated the carboxy-containing side chains into the 7α-position of the steroid scaffold and found that 17-keto derivative CH4893237 (12b) functioned as a pure antiestrogen with its oral activity much superior to clinically used pure antiestrogen, ICI182,780. Results from the pharmacokinetic evaluation indicated that the potent antiestrogen activity at oral dosing in mice attributed to both improved absorption from the intestinal wall and metabolic stability in liver.
Steroid derivatives bearing the carboxy moiety in the long side chain at the 7-α position exhibited remarkable antiestrogen activities when administered orally.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 16, Issue 18, 15 September 2006, Pages 4959–4964
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 16, Issue 18, 15 September 2006, Pages 4959–4964
نویسندگان
Yoshitake Kanbe, Myung-Hwa Kim, Masahiro Nishimoto, Yoshihito Ohtake, Takaaki Yoneya, Iwao Ohizumi, Toshiaki Tsunenari, Kenji Taniguchi, Shin-ichi Kaiho, Yoshiaki Nabuchi, Hiroshi Araya, Setsu Kawata, Kazumi Morikawa, Jae-Chon Jo, Hee-An Kwon,