کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
10592536 981794 2012 5 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Steroidal C-21 heteroaryl thioethers. Part 3: Pregn-4-eno-[3,2-c]pyrazole fused A ring modified steroids as selective glucocorticoid receptor modulators (dissociated steroids)
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Steroidal C-21 heteroaryl thioethers. Part 3: Pregn-4-eno-[3,2-c]pyrazole fused A ring modified steroids as selective glucocorticoid receptor modulators (dissociated steroids)
چکیده انگلیسی
The introduction of A ring pyrazole modification to the hydrocortisone C-21 heteroaryl thioethers generated compounds with excellent transrepression potency (IL-8 inhibition) compared to their hydrocortisone analogs. However, the transcriptional transactivation activity of these compounds were considerably higher than the corresponding hydrocortisone analogs. Among all the compounds evaluated, a quinoxaline thioether modification demonstrated the best overall in vitro separation.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 9, 1 May 2012, Pages 3291-3295
نویسندگان
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