کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1364164 981530 2009 5 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Design of novel quinazoline derivatives and related analogues as potent and selective ALK5 inhibitors
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Design of novel quinazoline derivatives and related analogues as potent and selective ALK5 inhibitors
چکیده انگلیسی

Starting from quinazoline 3a, we designed potent and selective ALK5 inhibitors over p38MAP kinase from a rational drug design approach based on co-crystal structures in the human ALK5 kinase domain. The quinazoline 3d exhibited also in vivo activity in an acute rat model of DMN-induced liver fibrosis when administered orally at 5 mg/kg (bid).

Starting from quinazoline 3a, we identified 3d a potent and selective ALK5 inhibitor over p38MAP kinase suitable for oral administration.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 8, 15 April 2009, Pages 2277–2281
نویسندگان
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