کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1397585 1501178 2011 5 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Design, synthesis, and biological evaluation of novel γ-carboline ketones as anticancer agents
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Design, synthesis, and biological evaluation of novel γ-carboline ketones as anticancer agents
چکیده انگلیسی

A series of novel γ-carboline ketones were designed, synthesized and evaluated for their cytotoxic activity in vitro against six human cancer cell lines (A549, SGC, HCT116, MCF-7, K562 and K562R). Biological evaluation revealed that almost all of the new compounds displayed moderate to potent cytotoxic activities against the tested cells. Among them, seven of the fourteen new compounds show more potent cytotoxic activities against K562R cell line than that of the positive control, taxol. Primary mechanism research on the most potent compound 6f indicated that it was a potent tubulin polymerization inhibitor, with IC50 value of 4.3 μM, equivalent to that of CA-4, and arresting cell cycle in G2/M phase.

A new series of γ-carboline ketones were designed, synthesized and evaluated for their cytotoxic activities, cell cycle effects, and tubulin polymerization inhibition.Figure optionsDownload as PowerPoint slideResearch highlights
► We designed and synthesized a new series of γ-carboline ketones.
► All the compounds were tested their cytotoxic activities in vitro against six human cancer cell lines including a multidrug resistant cell. Almost all of the new compounds displayed moderate to potent cytotoxic activities against the tested cells.
► The most potent compound 6f indicated that it was a potent tubulin polymerization inhibitor and arrested cell cycle in G2/M phase.

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: European Journal of Medicinal Chemistry - Volume 46, Issue 4, April 2011, Pages 1343–1347
نویسندگان
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