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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...

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Detalles Bibliográficos
Autores principales: Gaugaz, Fabienne Zdenka, Chicca, Andrea, Redondo-Horcajo, Mariano, Barasoain, Isabel, Díaz, J. Fernando, Altmann, Karl-Heinz
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2019
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6429585/
https://www.ncbi.nlm.nih.gov/pubmed/30841526
http://dx.doi.org/10.3390/ijms20051113