کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1358696 | 981359 | 2015 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Tetrahydropyrrolo-diazepenones as inhibitors of ERK2 kinase
دانلود مقاله + سفارش ترجمه
دانلود مقاله ISI انگلیسی
رایگان برای ایرانیان
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Tetrahydropyrrolo-diazepenones as inhibitors of ERK2 kinase Tetrahydropyrrolo-diazepenones as inhibitors of ERK2 kinase](/preview/png/1358696.png)
چکیده انگلیسی
A series of structure based drug design hypotheses and focused screening efforts led to the identification of tetrahydropyrrolo-diazepenones with striking potency against ERK2 kinase. The role of fluorination in mitigating microsomal clearance was systematically explored. Ultimately, it was found that fluorination of a cyclopentanol substructure provided significant improvement in both potency and human metabolic stability.
Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 25, Issue 18, 15 September 2015, Pages 3788–3792
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 25, Issue 18, 15 September 2015, Pages 3788–3792
نویسندگان
Jeffrey T. Bagdanoff, Rama Jain, Wooseok Han, Shejin Zhu, Ann-Marie Madiera, Patrick S. Lee, Xiaolei Ma, Daniel Poon,