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)
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس 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) 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)](/preview/png/10592536.png)
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
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 9, 1 May 2012, Pages 3291-3295
نویسندگان
Purakkattle Biju, Hongwu Wang, John Anthes, Kevin McCormick, Robert Aslanian, Michael Berlin, Rema Bitar, Yeon-Hee Lim, Yoon Joo Lee, Daniel Prelusky, Robbie Mcleod, Yanlin Jia, Xiomora Fernandez, Gissela Lieber, Johanna Jimenez, Steve Eckel,