Functional 1, 3a, 6a-triazapentalene scaffold: Design of fluorescent probes for kinesin spindle protein (KSP). Issue 23 (1st December 2016)

• Record Type: Journal Article
• Authors: Sawada, Jun-ichi; Osawa, Ayumi; Takeuchi, Tomoki; Kaneda, Masato; Oishi, Shinya; Fujii, Nobutaka; Asai, Akira; Tanino, Keiji; Namba, Kosuke
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 26:Issue 23(2016)
• Page Start: 5765
• Page End: 5769
• Publication Date: 2016-12-01
• Subjects: Kinesin spindle protein -- KSP -- Probe -- Triazapentalene; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2016.10.047
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: 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.