کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
10593994 981818 2011 4 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Discovery of amide replacements that improve activity and metabolic stability of a bis-amide smoothened antagonist hit
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Discovery of amide replacements that improve activity and metabolic stability of a bis-amide smoothened antagonist hit
چکیده انگلیسی
A bis-amide antagonist of Smoothened, a seven-transmembrane receptor in the Hedgehog signaling pathway, was discovered via high throughput screening. In vitro and in vivo experiments demonstrated that the bis-amide was susceptible to N-acyl transferase mediated amide scission. Several bioisosteric replacements of the labile amide that maintained in vitro potency were identified and shown to be metabolically stable in vitro and in vivo.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 18, 15 September 2011, Pages 5206-5209
نویسندگان
, , , , , , , , , , , , , , , , ,