Bioorganic & Medicinal Chemistry ( IF 3.3 ) Pub Date : 2020-05-19 , DOI: 10.1016/j.bmc.2020.115547 Manvendra Singh 1 , Nathan Garza 1 , Zachary Pearson 1 , Justin Douglas 2 , Zarko Boskovic 1
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A collection of small molecules has been synthesized by composing photo-cycloaddition, C–H functionalization, and N-capping strategies. Multidimensional biological fingerprints of molecules comprising this collection have been recorded as changes in cell and organelle morphology. This untargeted, phenotypic approach allowed for a broad assessment of biological activity to be determined. Reproducibility and the magnitude of measured fingerprints revealed activity of several treatments. Reactive functional groups, such as imines, dominated the observed activity. Two non-reactive candidate compounds with distinct bioactivity fingerprints were identified, as well.
中文翻译：
通过“细胞绘画”广泛评估了螺茚满吡咯烷的生物活性。
通过组成光环加成，CH功能化和N封端策略，已经合成了一系列小分子。包含该集合的分子的多维生物指纹已被记录为细胞和细胞器形态的变化。这种无针对性的表型方法可以确定广泛的生物学活性。再现性和所测指纹的大小显示了几种处理的活性。反应性官能团（例如亚胺）主导着观察到的活性。还鉴定了两种具有不同生物活性指纹的非反应性候选化合物。
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