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Epothilone A and B—Novel 16‐Membered Macrolides with Cytotoxic Activity: Isolation, Crystal Structure, and Conformation in Solution
512
Citations
3
References
1996
Year
Crystal StructureCytotoxic MacrolidesBiochemistryMedicineRational Drug DesignMicrobial Secondary MetabolitesNmr Spectroscopic ResultsSecondary MetabolitePrimary MetaboliteAntimicrobial CompoundCytotoxic ActivityPharmacologyPharmaceutical ChemistryBiomolecular EngineeringDrug DiscoveryB—novel 16‐MemberedDrug Resistance
How similar must a compound be to taxol in order to displace it from its binding site on microtubules? The microbial secondary metabolites epothilones A (1a) and B (1b) provide an answer to this question. These comparatively small, simply constructed, and highly cytotoxic macrolides surprisingly show no similarity to taxol, according to X-ray and NMR spectroscopic results.
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