کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1377713 981986 2006 5 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Discovery and structure–activity relationship of 2-phenyl-oxazole-4-carboxamide derivatives as potent apoptosis inducers
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Discovery and structure–activity relationship of 2-phenyl-oxazole-4-carboxamide derivatives as potent apoptosis inducers
چکیده انگلیسی

As a continuation of our efforts to discover novel apoptosis inducers as anticancer agents using a cell-based caspase HTS assay, 2-phenyl-oxazole-4-carboxamide derivatives were identified. The structure–activity relationships of this class of molecules were explored. Compound 1k, with EC50 of 270 nM and GI50 of 229 nM in human colorectal DLD-1 cells, was selected and demonstrated the ability to cleave PARP and displayed DNA laddering, the hallmarks of apoptosis. Compound 1k showed 63% tumor growth inhibition in human colorectal DLD-1 xenograft mouse model at 50 mpk, bid.

Novel 2-phenyl-oxazole-4-carboxamide-containing apoptosis inducers were discovered from a cell-based assay for caspase-3 activation. Synthesis, in vitro, and in vivo activity profiles are reported.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 16, Issue 17, 1 September 2006, Pages 4554–4558
نویسندگان
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