کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1369364 | 981775 | 2013 | 4 صفحه PDF | دانلود رایگان |
Eight novel 4,5-tetrahydropyrazolo[1,5-d][1,4]oxazepine derivatives have been synthesized and purified to be screened for anticancer activity. By a modified TRAP assay, some titled compounds were tested against telomerase, and compound 4a showed the most potent inhibitory activity with IC50 value at 0.78 ± 0.22 μM. Western blot assays showed that compounds 4a and 4b could inhibit expression of Cyclin D1, TERT, phospho-AKT and PI3K/AKT pathway.
Novel 4,5-tetrahydropyrazolo[1,5-d][1,4]oxazepine derivatives as potential telomerase inhibitors were synthesized. By a modified TRAP assay, some titled compounds were tested against telomerase, and compound 4a showed the most potent inhibitory activity with IC50 value at 0.78 ± 0.22 μM. Western blot assays showed that compound 4a could inhibit expression of Cyclin D1, TERT, phospho-AKT and PI3K/AKT pathway.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 23, Issue 3, 1 February 2013, Pages 720–723