Synthesis and Biological Evaluation of 7-Deoxy-Epothilone Analogues
AbstractThe synthesis of two deoxygenated analogues of potent epothilones is reported in an effort to analyze the relative importance of molecular conformation and ligand–target interactions to biological activity. 7-deoxy-epothilone D and 7-deoxy-(S)-14-methoxy-epothilone D were prepared through total synthesis and shown to maintain the conformational preferences of their biologically active parent congeners through computer modeling and nuclear magnetic resonance (NMR) studies. The significant decrease in observed potency for each compound suggests that a hydrogen bond between the C7-hydroxyl group and the tubulin binding site plays a critical role in the energetics of binding in the epothilone class of polyketides. View Full-Text
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Woods, L.M.; Arico, J.W.; Frein, J.D.; Sackett, D.L.; Taylor, R.E. Synthesis and Biological Evaluation of 7-Deoxy-Epothilone Analogues. Int. J. Mol. Sci. 2017, 18, 648.
Woods LM, Arico JW, Frein JD, Sackett DL, Taylor RE. Synthesis and Biological Evaluation of 7-Deoxy-Epothilone Analogues. International Journal of Molecular Sciences. 2017; 18(3):648.Chicago/Turabian Style
Woods, Laura M.; Arico, Joseph W.; Frein, Jeffrey D.; Sackett, Dan L.; Taylor, Richard E. 2017. "Synthesis and Biological Evaluation of 7-Deoxy-Epothilone Analogues." Int. J. Mol. Sci. 18, no. 3: 648.
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