کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1371428 981845 2011 5 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Synthesis and SAR of novel quinazolines as potent and brain-penetrant c-jun N-terminal kinase (JNK) Inhibitors
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Synthesis and SAR of novel quinazolines as potent and brain-penetrant c-jun N-terminal kinase (JNK) Inhibitors
چکیده انگلیسی

Quinazoline 3 was discovered as a novel c-jun N-terminal kinase (JNK) inhibitor with good brain penetration and pharmacokinetic (PK) properties. A number of analogs which were potent both in the biochemical and cellular assays were discovered. Quinazoline 13a was found to be a potent JNK3 inhibitor (IC50 = 40 nM), with >500-fold selectivity over p38, and had good PK and brain penetration properties. With these properties, 13a is considered a potential candidate for in vivo evaluation.

Quinazolines 3 and 13a were discovered as novel c-jun N-terminal kinase (JNK) inhibitors with good brain penetration and pharmacokinetic (PK) properties. Compound 13a is considered a potential candidate for in vivo evaluation.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 6, 15 March 2011, Pages 1719–1723
نویسندگان
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