کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
10590989 981734 2014 6 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Synthesis and structure-activity relationship of non-peptidic antagonists of neuropilin-1 receptor
ترجمه فارسی عنوان
سنتز و ارتباط ساختار-فعالیت غیر آنتی بادیهای پپتییدی گیرنده نوروپیلین-1
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
چکیده انگلیسی
Neuropilins (NRPs) are VEGF-A165 co-receptors over-expressed in tumor cells, and considered as targets in angiogenic-related pathologies. We previously identified compound 1, the first non-peptidic antagonist of the VEGF-A165/NRP binding, which exhibits in vivo anti-angiogenic and anti-tumor activities. We report here the synthesis and biological evaluations of new antagonists structurally-related to compound 1. Among these molecules, 4a, 4c and 4d show cytotoxic effects on HUVEC and MDA-MB-31 cells, and antagonize VEGF-A165/NRP-1 binding. This study confirmed our key structure-activity relationships hypothesis and paved the way to compound 1 'hit to lead' optimization.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 24, Issue 17, 1 September 2014, Pages 4254-4259
نویسندگان
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