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Cover Picture: Making Epothilones Fluoresce: Design, Synthesis, and Biological Characterization of a Fluorescent N12-Aza-Epothilone (Azathilone) (ChemBioChem 15/2009)

✍ Scribed by Jürg Gertsch ; Fabian Feyen ; Alexander Bützberger; Barbara Gerber; Bernhard Pfeiffer; Karl-Heinz Altmann

Publisher: John Wiley and Sons
Year: 2009
Tongue: English
Weight: 980 KB
Volume: 10
Category: Article
ISSN: 1439-4227
DOI: 10.1002/cbic.200990065

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✦ Synopsis

The cover picture shows cells with a green fluorescent microtubule network after treatment with the fluorescent epothilone analogue NBD-azathilone. Docking studies indicate that the NBD moiety of the tubulin-bound analogue is located in a hydrophobic pocket that is not utilized by natural epothilones and directly contributes to tubulin binding. For further information on elucidating the binding and cellular effects of this analogue, see the article by K. H. Altmann et al. on p. 2513 ff.

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Making Epothilones Fluoresce: Design, Sy

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

✍ Jürg Gertsch ; Fabian Feyen ; Alexander Bützberger; Barbara Gerber; Bernhard Pfe 📂 Article 📅 2009 🏛 John Wiley and Sons 🌐 English ⚖ 907 KB

## Abstract __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