Making Epothilones Fluoresce: Design, Synthesis, and Biological Characterization of a Fluorescent N12-Aza-Epothilone (Azathilone)

A green fluorescent 12-aza-epothilone (azathilone) derivative has been prepared through the attachment of the 4-nitro-2,1,3-benzoxadiazole (NBD) fluorophore to the 12-nitrogen atom of the azamacrolide core structure. While less potent than natural epothilones or different N12-acylated azathilone der...

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Veröffentlicht in:	Chembiochem : a European journal of chemical biology 2009-10, Vol.10 (15), p.2513-2521
Hauptverfasser:	Gertsch, Jürg, Feyen, Fabian, Bützberger, Alexander, Gerber, Barbara, Pfeiffer, Bernhard, Altmann, Karl-Heinz
Format:	Artikel
Sprache:	eng
Schlagworte:	4-Chloro-7-nitrobenzofurazan - analogs & derivatives 4-Chloro-7-nitrobenzofurazan - chemical synthesis 4-Chloro-7-nitrobenzofurazan - chemistry 4-Chloro-7-nitrobenzofurazan - metabolism 4-Chloro-7-nitrobenzofurazan - pharmacology azathilone Binding Sites biological activity Cell Cycle - drug effects Cell Line, Tumor Cell Proliferation - drug effects Drug Design epothilone Epothilones - chemical synthesis Epothilones - chemistry Epothilones - metabolism Epothilones - pharmacology Fluorescence Fluorescent Dyes - chemical synthesis Fluorescent Dyes - chemistry Fluorescent Dyes - metabolism Fluorescent Dyes - pharmacology fluorescent probes Humans microtubules Microtubules - metabolism Spectrum Analysis Tubulin - metabolism
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