Broad assessment of bioactivity of a collection of spiroindane pyrrolidines through "cell painting".

Manvendra Singh, Nathan Garza, Zachary Pearson, Justin Douglas, Zarko Boskovic

Bioorganic & medicinal chemistry 2020 Jul 01

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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. Copyright © 2020 Elsevier Ltd. All rights reserved.

Citation

Manvendra Singh, Nathan Garza, Zachary Pearson, Justin Douglas, Zarko Boskovic. Broad assessment of bioactivity of a collection of spiroindane pyrrolidines through "cell painting". Bioorganic & medicinal chemistry. 2020 Jul 01;28(13):115547