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Translational synthetic chemistry

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Providing chemical matter to modulate newly identified biological targets—as well as pre-existing but chemically intractable ones—remains a challenge in the discovery of therapeutics. Here, we discuss opportunities for synthetic chemists to make a direct impact in addressing targets that are considered 'undruggable'.

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Figure 1: Synthetic methodology enabling the efficient production of bioactive natural products.
Figure 2: Recent synthetic methodology useful for library generation and compound optimization.
Figure 3: The interplay among natural products, fragment-based approaches and natural product (NP)–inspired library generation.

References

  1. Austad, B.C. et al. Synlett 24, 333–337 (2013).

    Article  CAS  Google Scholar 

  2. Shi, J. et al. J. Am. Chem. Soc. 133, 8014–8027 (2011).

    Article  CAS  Google Scholar 

  3. Mousseau, G. et al. Cell Host Microbe 12, 97–108 (2012).

    Article  CAS  Google Scholar 

  4. Hegde, N.S., Sanders, D.A., Rodriguez, R. & Balasubramanian, S. Nat. Chem. 3, 725–731 (2011).

    Article  CAS  Google Scholar 

  5. O' Connor, C.J., Beckmann, H.S.G. & Spring, D.R. Chem. Soc. Rev. 41, 4444–4456 (2012).

    Article  CAS  Google Scholar 

  6. Marcaurelle, L.A., Johannes, C., Yohannes, D., Tillotson, B.P. & Mann, D. Bioorg. Med. Chem. Lett. 19, 2500–2503 (2009).

    Article  CAS  Google Scholar 

  7. Heidebrecht, R.W. Jr. et al. ACS Med. Chem. Lett. 3, 112–117 (2012).

    Article  CAS  Google Scholar 

  8. Walji, A.M. & MacMillan, D.W.C. Synlett. 2007, 1477–1489 (2007).

    Article  Google Scholar 

  9. Zhou, H. et al. J. Med. Chem. doi:10.1021/jm3015298 (17 January 2013).

  10. Marcaurelle, L.A. et al. J. Am. Chem. Soc. 132, 16962–16976 (2010).

    Article  Google Scholar 

  11. Hili, R., Rai, V. & Yudin, A.K. J. Am. Chem. Soc. 132, 2889–2891 (2010).

    Article  CAS  Google Scholar 

  12. Bachovchin, D.A. et al. Proc. Natl. Acad. Sci. USA 108, 6811–6816 (2011).

    Article  CAS  Google Scholar 

  13. Schulz, M.N. & Hubbard, R.E. Curr. Opin. Pharmacol. 9, 615–621 (2009).

    Article  CAS  Google Scholar 

  14. Sun, Q. et al. Angew. Chem. Int. Ed. Engl. 51, 6140–6143 (2012).

    Article  CAS  Google Scholar 

  15. Maurer, T. et al. Proc. Natl. Acad. Sci. USA 109, 5299–5304 (2012).

    Article  CAS  Google Scholar 

  16. Bamborough, P. et al. J. Med. Chem. 55, 587–596 (2012).

    Article  CAS  Google Scholar 

  17. Dai, H.-X., Stepan, A.F., Plummer, M.S., Zhang, Y.-H. & Yu, J.-Q. J. Am. Chem. Soc. 133, 7222–7228 (2011).

    Article  CAS  Google Scholar 

  18. Over, B. et al. Nat. Chem. 5, 21–28 (2013).

    Article  CAS  Google Scholar 

  19. Hung, A.W. et al. Proc. Natl. Acad. Sci. USA 108, 6799–6804 (2011).

    Article  CAS  Google Scholar 

  20. Hajduk, P.J., Galloway, W.R. & Spring, D.R. Nature 470, 42–43 (2011).

    Article  CAS  Google Scholar 

  21. Verdine, G.L. & Hilinski, G.J. Drug Discov. Today. Technol. 9, e41–e47 (2012).

    Article  CAS  Google Scholar 

  22. Bernal, F. et al. Cancer Cell 18, 411–422 (2010).

    Article  CAS  Google Scholar 

  23. Grossmann, T.N. et al. Proc. Natl. Acad. Sci. USA 109, 17942–17947 (2012).

    Article  CAS  Google Scholar 

  24. Madden, M.M. et al. Bioorg. Med. Chem. Lett. 21, 1472–1475 (2011).

    Article  CAS  Google Scholar 

  25. Yan, C. & Higgins, P.J. Biochim. Biophys. Acta 1835, 76–85 (2013).

    CAS  PubMed  Google Scholar 

  26. Clemons, P.A. et al. Proc. Natl. Acad. Sci. USA 108, 6817–6822 (2011).

    Article  CAS  Google Scholar 

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Correspondence to Lisa A Marcaurelle.

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Kesavan, S., Marcaurelle, L. Translational synthetic chemistry. Nat Chem Biol 9, 210–213 (2013). https://doi.org/10.1038/nchembio.1207

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