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对吲哚 - 3 - 甲醇及相关片段的初步构效关系研究揭示了一种针对耐药性胶质母细胞瘤细胞的新型抗癌先导化合物。

Preliminary SAR on indole-3-carbinol and related fragments reveals a novel anticancer lead compound against resistant glioblastoma cells.

作者信息

Sherer Christopher, Tolaymat Ibrahim, Rowther Farzana, Warr Tracy, Snape Timothy J

机构信息

School of Pharmacy and Biomedical Sciences, University of Central Lancashire, Maudland Building, Preston, Lancashire PR1 2HE, UK.

Faculty of Medical Science, Anglia Ruskin University, Bishop Hall Lane, Chelmsford, Essex CM1 1SQ, UK.

出版信息

Bioorg Med Chem Lett. 2017 Apr 1;27(7):1561-1565. doi: 10.1016/j.bmcl.2017.02.033. Epub 2017 Feb 17.

Abstract

The prognosis for glioblastoma patients is, at best, poor, with the median time of survival after diagnosis measured in months. As such, there is much need for the rapid development of potent and novel treatments. Herein, we report our preliminary findings on the SAR of a series of indole-3-carbinol and related fragments and reveal a potent lead with low micromolar activity against a particularly resistant glioblastoma cell culture, providing a new platform for future development of a new therapy in this area.

摘要

胶质母细胞瘤患者的预后充其量也很差,诊断后的中位生存时间以月计算。因此,迫切需要快速开发有效的新型治疗方法。在此,我们报告了一系列吲哚 - 3 - 甲醇及其相关片段的构效关系的初步研究结果,并揭示了一种对一种特别耐药的胶质母细胞瘤细胞培养具有低微摩尔活性的有效先导化合物,为该领域新疗法的未来发展提供了一个新平台。

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