Identification of a new natural camptothecin analogue in targeted screening for HIF-1α inhibitors
Identification of a new natural camptothecin analogue in targeted screening for HIF-1α inhibitors
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DOI：
10.1055/s-2006-951767
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发表时间：
2007-01-01
期刊：
影响因子：
2.7
通讯作者：
Shoemaker, Robert H.
中科院分区：
文献类型：
--
作者：
Klausmeyer, Paul;McCloud, Thomas G.;Shoemaker, Robert H.
筛选以检测抑制HIF-1 a转录激活途径的化合物，鉴定了蛇根草提取物用于研究。采用高通量去复制策略，包括色谱法，通过生物活性测试和文献参考支持光谱数据采集，这导致快速鉴定喜树碱（1）和三种类似物（2-4）作为活性化合物。9，10-亚甲二氧基-（20 S）-喜树碱（4）为首次从植物中发现。
Screening to detect compounds that inhibit the HIF-1 a transcriptional activation pathway identified an extract of Ophiorrhiza trichocarpon for investigation. A high throughput dereplication strategy was employed, involving chromatography with spectral data acquisition supported by bioactivity testing and literature referencing, which led to rapid identification of camptothecin (1) and three analogues (2-4) as the active compounds. 9,10-Methylenedioxy-(20S)-camptothecin (4) was found for the first time from a plant.