کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
2028638 | 1070432 | 2009 | 6 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
6β,19-Bridged androstenedione analogs as aromatase inhibitors
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کلمات کلیدی
موضوعات مرتبط
علوم زیستی و بیوفناوری
بیوشیمی، ژنتیک و زیست شناسی مولکولی
زیست شیمی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: 6β,19-Bridged androstenedione analogs as aromatase inhibitors 6β,19-Bridged androstenedione analogs as aromatase inhibitors](/preview/png/2028638.png)
چکیده انگلیسی
Inhibition of aromatase is an efficient approach for the prevention and treatment of breast cancer. New 6β,19-bridged steroid analogs of androstenedione, 6β,19-epithio- and 6β,19-methano compounds 11 and 17, were synthesized starting from 19-hydroxyandrostenedione (6) and 19-formylandrost-5-ene-3β,17β-yl diacetate (12), respectively, as aromatase inhibitors. All of the compounds including known steroids 6β,19-epoxyandrostenedione (4) and 6β,19-cycloandrostenedione (5) tested were weak to poor competitive inhibitors of aromatase and, among them, 6β,19-epoxy steroid 4 provided only moderate inhibition (Ki: 2.2 μM). These results show that the 6β,19-bridged groups of the inhibitors interfere with binding in active site of aromatase.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Steroids - Volume 74, Issue 12, 4 November 2009, Pages 884–889
Journal: Steroids - Volume 74, Issue 12, 4 November 2009, Pages 884–889
نویسندگان
Sachiko Komatsu, Ayaka Yaguchi, Kouwa Yamashita, Masao Nagaoka, Mitsuteru Numazawa,