Total Synthesis of an Epothilone Analogue based on the Amide‒Triazole Bioisosterism.
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DOI: 10.1002/cplu.202400413
Abstract: Epothilones are 16-membered macrolides that can act as microtubule-targeting agents to tackle cancer. Many synthetic analogues have been investigated for their activity, yet often based on macrolide structures. A notable exception is Ixabepilone, an azalide… read more here.
Keywords: total synthesis; amide triazole; epothilone; triazole bioisosterism ... See more keywords
Epothilone D Modulates Autism-like Behaviors in the BTBR Mouse Model of Autism Spectrum Disorder
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DOI: 10.1016/j.neuroscience.2022.02.025
Abstract: Autism spectrum disorder (ASD) is a neurodevelopmental disorder, characterized by impaired social communication, abnormal repetitive behaviors and restricted interests and/or sensory behaviors. It has been widely accepted that ASD involves a complex interplay of both… read more here.
Keywords: epothilone; autism spectrum; autism; behaviors btbr ... See more keywords
Synthesis, Microtubule-Binding Affinity, and Antiproliferative Activity of New Epothilone Analogs and of an EGFR-Targeted Epothilone-Peptide Conjugate
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DOI: 10.3390/ijms20051113
Abstract: 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… read more here.
Keywords: epothilone; conjugate; affinity; microtubule binding ... See more keywords