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

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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Bibliographic Details
Main Authors: Fabienne Zdenka Gaugaz, Andrea Chicca, Mariano Redondo-Horcajo, Isabel Barasoain, J. Fernando Díaz, Karl-Heinz Altmann
Format: Article
Language:English
Published: MDPI AG 2019-03-01
Series:International Journal of Molecular Sciences
Subjects:
cancer
drug discovery
epothilone
medicinal chemistry
microtubule-stabilizing agents
prodrug
total synthesis
tumor-targeting
Online Access:http://www.mdpi.com/1422-0067/20/5/1113

Internet

http://www.mdpi.com/1422-0067/20/5/1113

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