کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1357918 981304 2014 7 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Synthesis of pyrazolo[4,3-a]phenanthridines, a new scaffold for Pim kinase inhibition
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Synthesis of pyrazolo[4,3-a]phenanthridines, a new scaffold for Pim kinase inhibition
چکیده انگلیسی

A new series of nitro or amino substituted pyrazolo[4,3-a]phenanthridines was synthesized in 6 steps from 5-bromo-6-nitroindazole. The evaluation of their inhibitory potency toward Pim kinases demonstrated that the nitro series could be considered as an interesting starting point for the development of new Pim kinase inhibitors, especially Pim-3. A preferential binding mode was suggested by molecular modeling experiments for nitro series and Pim-1/Pim-3 ATP-binding sites. Moreover, the most active compounds exhibited antiproliferative activities toward PC3 cells in the micromolar range.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 22, Issue 17, 1 September 2014, Pages 4704–4710
نویسندگان
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