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

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• 作者：Jun-ichi Sawada^a ; ^&dagger ; ; Ayumi Osawa^b ; ^c ; ^&dagger ; ; Tomoki Takeuchi^d ; Masato Kaneda^d ; Shinya Oishi^d ; ^{soishi@pharm.kyoto-u.ac.jp" class="auth_mail" title="E-mail the corresponding author} ; Nobutaka Fujii^d ; Akira Asai^a ; ^{aasai@u-shizuoka-ken.ac.jp" class="auth_mail" title="E-mail the corresponding author} ; Keiji Tanino^e ; Kosuke Namba^b ; ^e
• 关键词：Kinesin spindle protein ; KSP ; Probe ; Triazapentalene
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2016
• 出版时间：1 December 2016
• 年：2016
• 卷：26
• 期：23
• 页码：5765-5769
• 全文大小：1203 K

文摘

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.