Synthesis, Biological Profiling and Determination of the Tubulin-Bound Conformation of 12-Aza-Epothilones (Azathilones)

Synthesis, Biological Profiling and Determination of the Tubulin-Bound Conformation of 12-Aza-Epothilones (Azathilones)

12-Aza-epothilones (azathilones) incorporating quinoline side chains and bearing different N12-substituents have been synthesized via highly efficient RCM-based macrocyclizations. Quinoline-based azathilones with the side chain N-atom in the meta-position to the C15 atom in the macrocycle are highly...

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Bibliographic Details
Main Authors: Andrea Jantsch, Lidia Nieto, Jürg Gertsch, Javier Rodríguez-Salarichs, Ruth Matesanz, Jesús Jiménez-Barbero, J. Fernando Díaz, Ángeles Canales, Karl-Heinz Altmann
Format: Article
Language:English
Published: MDPI AG 2016-08-01
Series:Molecules
Subjects:
anticancer
azathilones
conformation
drug discovery
epothilones
natural product
SAR
STD
synthesis
tubulin
Online Access:http://www.mdpi.com/1420-3049/21/8/1010

Internet

http://www.mdpi.com/1420-3049/21/8/1010

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