期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 27, 期 14, 页码 3092-3095出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2017.05.046
关键词
Benzoxazin-5-one; Anti-proliferative activity; Suzuki-Miyaura cross coupling; Cell cycle analysis; Cancer cell lines
In this study, we investigate the anti-proliferative activity of a small library of 7-substituted 5H-pyrrolo [1,2-a][3,1]benzoxazin-5-one derivatives, against a panel of human cancer cell lines. We reported the synthesis of these compounds in a previous work. 7-Bromo-5H-benzo[d]pyrrolo[2,1-b][1,3]oxazin-5-one showed a promising anti-proliferative effect. As starting material for Suzuki-Miyaura cross coupling reaction, it was selected for the design and the synthesis of six further derivatives, with the aim to better define structure-activity relationships. The anti-proliferative MTT assay revealed a dose-dependent reduction of cell viability, especially for 7-([1,1'-biphenyl]-4-yl)-5H-benzo[d]pyrrolo[2,1-b][1,3]oxazin5-one. Cell cycle and western blotting analysis suggested apoptosis as possible mechanism for its anti proliferative activity. These preliminary results encourage our interest for further optimizations. (C) 2017 Elsevier Ltd. All rights reserved.
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