Abstract
AbstractThe fraction of sp3‐hybdrised carbons (Fsp3) in drug candidates and other biologically relevant compounds has been proposed to be an important physicochemical consideration within medicinal chemistry. Currently available small‐molecule probes for Raman imaging are not optimised for biological applications. We sought to improve upon the highly Raman‐active, yet rigid, lipophilic, and aggregative, bisarylbutadiyne (BADY) motif by introducing Fsp3 character. BADY analogues were designed, efficiently synthesised, and analysed by mass spectrometry – revealing a statistical correlation between compound aggregation and cLogP, but no correlation with Fsp3. However, X‐ray crystallography demonstrated that the modifications to the BADY structure had a marked effect on crystal packing, suggesting Fsp3 may still be important in reducing intermolecular stacking, and thus aggregation, of BADY. Cellular imaging by stimulated Raman scattering (SRS) microscopy allowed comparison of the intracellular distribution of the tags, guiding the design of future Raman probes.
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