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Synthesis, Microtubule-Binding Affinity, and Antiproliferative Activity of New Epothilone Analogs and of an EGFR-Targeted Epothilone-Peptide Conjugate

A new simplified, epoxide-free epothilone analog was prepared incorporating an N-(2-hydroxyethyl)-benzimidazole side chain, which binds to microtubules with high affinity and inhibits cancer cell growth in vitro with nM potency. Building on this scaffold, a disulfide-linked conjugate with the purpor...

Ausführliche Beschreibung

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Bibliographische Detailangaben
Veröffentlicht in:Int J Mol Sci
Hauptverfasser: Gaugaz, Fabienne Zdenka, Chicca, Andrea, Redondo-Horcajo, Mariano, Barasoain, Isabel, Díaz, J. Fernando, Altmann, Karl-Heinz
Format: Artigo
Sprache:Inglês
Veröffentlicht: MDPI 2019
Schlagworte:
Online Zugang:https://ncbi.nlm.nih.gov/pmc/articles/PMC6429585/
https://ncbi.nlm.nih.gov/pubmed/30841526
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.3390/ijms20051113
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