کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
10584554 981334 2013 11 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
A 2,6,9-hetero-trisubstituted purine inhibitor exhibits potent biological effects against multiple myeloma cells
ترجمه فارسی عنوان
مهار کننده پورین 2،6،9 هتروتیزه شده اثرات بیولوژیکی قوی بر روی سلول های چندتایی میلوم دارد
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
چکیده انگلیسی
A focused library of hetero-trisubstituted purines was developed for improving the cell penetrating and biological efficacy of a series of anti-Stat3 protein inhibitors. From this SAR study, lead agent 22e was identified as being a promising inhibitor of MM tumour cells (IC50's <5 μM). Surprisingly, biophysical and biochemical characterization proved that 22e was not a Stat3 inhibitor. Initial screening against the kinome, prompted by the purine scaffold's history for targeting ATP binding pockets, suggests possible targeting of the JAK family kinases, as well for ABL1 (nonphosphorylated F317L) and AAK1.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 21, Issue 17, 1 September 2013, Pages 5618-5628
نویسندگان
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