Functional 1,3a,6a-triazapentalene scaffold: Design of fluorescent probes for kinesin spindle protein (KSP)

Jun-Ichi Sawada,Ayumi Osawa,Tomoki Takeuchi,Masato Kaneda,Shinya Oishi,Nobutaka Fujii,Akira Asai,Keiji Tanino,Kosuke Namba

doi:10.1016/j.bmcl.2016.10.047

Functional 1,3a,6a-triazapentalene scaffold: Design of fluorescent probes for kinesin spindle protein (KSP)

Jun-Ichi Sawada, Ayumi Osawa + Show 7 more

https://doi.org/10.1016/j.bmcl.2016.10.047

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Journal: Bioorganic & Medicinal Chemistry Letters	Publication Date: Oct 15, 2016
Citations: 21

Affiliation: Tokushima University, Hokkaido University, Kyoto University, University of Shizuoka

#Kinesin Spindle Protein #Inhibitors Of Kinesin Spindle Protein + Show 8 more

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Abstract

1,3a,6a-Triazapentalene is a compact fluorescent chromophore. In this study, triazapentalene was used to modify a series of biphenyl-type inhibitors of kinesin spindle protein (KSP) to develop fluorescent probes for the intracellular visualization of this protein. Microscopic studies demonstrated that these novel triazapentalene-labeled compounds exhibited inhibitory activity towards KSP in cultured cells and provided important information concerning the intracellular distribution.

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