More About The Derek Tan Lab Minus iconIcon indicating subtraction, or that the element can be closed. Plus IconIcon indicating addition, or that the element can be opened. Arrow (down) icon.An arrow icon, usually indicating that the containing element can be opened and closed.

Complete Publications (Graphical Abstracts)

Read up on the latest publications in diversity-oriented synthesis, rational drug design, chemical biology, and drug discovery research from the Tan Lab!

Selected Publications: Text Only | Graphical Abstracts
Complete Publications: Text Only | Graphical Abstracts

Full-text versions of articles are available from the publisher with online journal subscription. PubMed Central (PMC) versions of articles are available free of charge.


2017 |  2016 |  2015 | 2014 | 2013 | 2012 | 2011 | 2010 | 2009 | 2008 | 2007 | 2006 | 2005 | 2004 | 2003 | 2002 | Postdoctoral | Graduate | Undergraduate ]




Tan Lab Publications

  1. Family-level stereoselective synthesis and biological evaluation of pyrrolomorpholine spiroketal natural product antioxidants
    Verano, A. L.; Tan, D. S.* Chem. Sci. 2017, 8, 3687–3693.
    Abstract | PubMed | PMC ] Chemical Science 2017 graphical abstract

  2. Stereocontrolled Synthesis of Spiroketals: An Engine for Chemical and Biological Discovery
    Verano, A. L.; Tan, D. S.* Isr. J. Chem. 2017, 57, 279–291.
    Abstract | PubMed | PMC ] Israel Journal of Chemistry 2017 graphical abstract

  3. Diastereoselective synthesis of highly substituted tetrahydrofurans by Pd-catalyzed tandem oxidative cyclization-redox relay reactions controlled by intramolecular hydrogen bonding.
    Brooks, J. L.; Xu, L.; Wiest, O.; Tan, D. S.* J. Org. Chem. 2017, 82, 57–75.
    Abstract | PubMed | PMC ] J. Org. Chem. 2017 graphical abstract

  4. Stereoselective synthesis, docking, and biological evaluation of difluoroindanediol-based MenE inhibitors as antibiotics.
    Evans, C. E.; Matarlo, J. S.; Tonge, P. J.*; Tan, D. S.* Org. Lett. 2016, 18, 6384–6387.
    Abstract | PubMed | PMC ] Org. Lett. 2016 graphical abstract

  5. Design, synthesis, and biological evaluation of α-hydroxyacyl-AMS inhibitors of amino acid adenylation enzymes.
    Davis, T. D.; Mohandas, P. ; Chiriac, M. I.; Bythrow, G. V.; Quadri, L. E. N.*; Tan, D. S.* Bioorg. Med. Chem. Lett. 2016, 21, 5340–5345.
    Abstract | PubMed | PMC ]  Bioorg. Med. Chem. Lett. 2016 graphical abstract

  6. Designed small-molecule inhibitors of the anthranilyl-CoA synthetase PqsA block quinolone biosynthesis in Pseudomonas aeruginosa.
    Ji, C.; Sharma, I.; Pratihar, I.; Hudson, L.; Maura, D.; Guney, T.; Rahme, L. G.; Pesci, E. C.; Coleman, J. P.; Tan, D. S.* ACS Chem. Biol. 2016, 11, 3061–3067.
    Abstract | PubMed | PMC ]
     ACS Chem. Biol 2016 graphical abstract

  7. Mechanism of MenE inhibition by acyl-adenylate analogues and discovery of novel antibacterial agents.
    Matarlo, J. S.; Evans, C. E.; Sharma, I.; Lavaud, L. J.; Ngo, S. C.; Shek, R.; Rajashankar, K. R.; French, J. B.; Tan, D. S.*; Tonge, P. J.* Biochemistry 2015, 54, 6514–6524.
    Abstract | PubMed | PMC ]
    Biochemistry 2015 graphical abstract

  8. Cheminformatic comparison of approved drugs from natural product versus synthetic origins.
    Stratton, C. F.; Newman, D. J.; Tan, D. S.* Bioorg. Med. Chem. Lett. 2015, 25, 4802–4807.
    Abstract | PubMed | PMC ]
    Bioorganic and Medicinal Chemistry Letters 2015 graphical abstract

  9. Principal component analysis as a tool for library design: A case study investigating natural products, brand-name drugs, natural product-like libraries, and drug-like libraries.
    Wenderski, T. A.; Stratton, C. F.; Bauer, R. A.; Kopp, F.; Tan, D. S.* Methods Mol. Biol. 2015, 1263, 225–242.
    Abstract | PubMed | PMC ]
    Methods in Molecular Biology 2015 graphical abstract

  10. General platform for systematic quantitative evaluation of small-molecule permeability in bacteria.
    Davis, T. D.; Gerry, C. J.; Tan, D. S.* ACS Chem. Biol. 2014, 9, 2535–2544.
    Abstract | PubMed | PMC ]
    ACS Chemical Biology 2014 graphical abstract

    (Highlighted in ACS Chem. Biol.)

  11. Solvent-dependent divergent functions of Sc(OTf)3 in stereoselective epoxide-opening spiroketalizations.
    Sharma, I.; Wurst, J. M.; Tan, D. S.* Org. Lett. 2014, 16, 2474–2477.
    Abstract | PubMed | PMC ]
    Organic Letters 2014 graphical abstract

  12. Pharmacokinetic and in vivo efficacy studies of the mycobactin biosynthesis inhibitor salicyl-AMS in mice.
    Lun, S.; Guo, H.; Adamson, J.; Cisar, J. S.; Davis, T. D.; Sundaramn Chavadi, S.; Warren, J. D.; Quadri, L. E. N.*; Tan, D. S.*; Bishai, W. R.* Antimicrob. Agents Chemother. 2013, 57, 5138–5140.
    Abstract | PubMed | PMC ]
    Antimicrobial Agents and Chemotherapy 2013 graphical abstract

  13. Diversifying complexity.
    Sharma, I.; Tan, D. S.* Nat. Chem. 2013, 5, 157–158.
    Abstract | PubMed  ]
    Nature Chemistry 2013 graphical abstract

  14. Biomimetic diversity-oriented synthesis of benzannulated medium rings via ring expansion.
    Bauer, R. A.; Wenderski, T. A.; Tan, D. S.* Nat. Chem. Biol. 2013, 9, 21–29.
    Abstract | PubMed | PMC ]
    Nature Chemical Biology 2013 graphical abstract

  15. Stereoselective synthesis of acortatarins A and B.
    Wurst, J. M.; Verano, A. L.; Tan, D. S.* Org. Lett. 2012, 14, 4442–4445.
    Abstract | PubMed | PMC ]
    Organic Letters 2012 graphical abstract

  16. A diversity-oriented synthesis approach to macrocycles via oxidative ring expansion.
    Kopp, F.; Stratton, C. F.; Akella, L. B.; Tan, D. S.* Nat. Chem. Biol. 2012, 8, 358–365.
    Abstract | PubMed | PMC ]
    Nature Chemical Biology 2012 graphical abstract

    (Highlighted in SciBX )

  17. Stable analogues of OSB-AMP: Potent inhibitors of MenE, the o-succinylbenzoate-CoA synthetase from bacterial menaquninone biosynthesis.
    Lu, X.; Zhou, R.; Sharma, I.; Li, X.; Kumar, G.; Swaminathan, S.; Tonge, P. J.*; Tan, D. S.* ChemBioChem 2012, 13, 129–136.
    Abstract | PubMed | PMC ]
    ChemBioChem 2012 graphical abstract

  18. Hydrogen-bonding catalysis and inhibition by simple solvents in the stereoselective kinetic epoxide-opening spirocyclization of glycal epoxides to form spiroketals.
    Wurst, J. M.; Liu, G.; Tan, D. S.* J. Am. Chem. Soc. 2011, 133, 7916–7925.
    Abstract | PubMed | PMC ]
    Journal of the American Chemical Society 2011 graphical abstract

  19. Solid-phase synthesis and chemical space analysis of a 190-membered alkaloid/terpenoid-like library.
    Moura-Letts, G.; DiBlasi, C. M.; Bauer, R. A.; Tan, D. S.* Proc. Natl. Acad. Sci. USA 2011, 108, 6745–6750.
    Abstract | PubMed | PMC ]
    Proceedings of the National Academy of Science USA 2011 graphical abstract

  20. The tert-butylsulfinamide lynchpin in transition-metal-mediated multiscaffold library synthesis.
    Bauer, R. A.; DiBlasi, C. M.; Tan, D. S.* Org. Lett. 2010, 12, 2084–2087.
    Abstract | PubMed | PMC ]
    Organic Letters 2010 graphical abstract

  21. Expanding the range of ’druggable’ targets with natural product-based libraries: An academic perspective.
    Bauer, R. A.; Wurst, J. M.; Tan, D. S.* Curr. Opin. Chem. Biol. 2010, 14, 308–314.
    Abstract | PubMed | PMC ]
    Current Opinion in Chemical Biology 2010 graphical abstract

  22. Active site remodelling accompanies thioester bond formation in the SUMO E1.
    Olsen, S. K.; Capili. A. D.; Lu, X.; Tan, D. S.*; Lima, C. D.* Nature 2010, 463, 906–912.
    Abstract | PubMed | PMC ]
    Nature 2010 graphical abstract

    (Highlighted in Nature, Chem. Eng. News, Nat. Rev. Mol. Cell Biol., Nat. Chem. Biol., Structure, ACS Chem. Biol., and Faculty of 1000 Biology )

  23. Designed semisynthetic protein inhibitors of Ub/Ubl E1 activating enzymes.
    Lu, X.; Olsen, S. K.; Capili, A. D.; Cisar, J. S.; Lima, C. D.*; Tan, D. S.* J. Am. Chem. Soc. 2010, 132, 1748–1749.
    Abstract | PubMed | PMC ]
    Journal of the American Chemical Society 2010 graphical abstract

    (Highlighted in Chem. Eng. News, Nat. Rev. Mol. Cell Biol., ACS Chem. Biol., and Faculty of 1000 Biology )

  24. Stereoselective synthesis of benzannulated spiroketals: Influence of the aromatic ring on reactivity and conformation.
    Liu, G.; Wurst, J. M.; Tan, D. S.* Org. Lett. 2009, 11, 3670–3673.
    Abstract | PubMed | PMC ]
    Organic Letters 2009 graphical abstract

  25. Mechanism-based inhibitors of MenE, an acyl-CoA synthetase involved in bacterial menaquinone biosynthesis.
    Lu, X.; Zhang, H.; Tonge, P. J.*; Tan, D. S.* Bioorg. Med. Chem. Lett. 2008, 18, 5963–5966.
    Abstract | PubMed | PMC ]
    Bioorganic and Medicinal Chemistry Letters 2008 graphical abstract

  26. Small molecule inhibition of microbial natural product biosynthesis – An emerging antibiotic strategy.
    Cisar, J. S.; Tan, D. S.* Chem. Soc. Rev. 2008, 37, 1320–1329.
    Abstract | PubMed | PMC ]
    Chemical Society Reviews 2008 graphical abstract

  27. Mycobacterial phenolic glycolipid virulence factor biosynthesis: Mechanism and small-molecule inhibition of polyketide chain initiation.
    Ferreras, J. A.; Stirrett, K. L.; Lu, X.; Ryu, J.-S.; Soll, C. E.; Tan, D. S.; Quadri, L. E. N.* Chem. Biol. 2008, 15, 51–61.
    Abstract | PubMed | PMC ]
    Chemical Biology 2008 graphical abstract

    (Highlighted in Chem. Biol. )

  28. Exploiting ligand conformation in selective inhibition of non-ribosomal peptide synthetase amino acid adenylation with designed macrocyclic small molecules.
    Cisar, J. S.; Ferreras, J. A.; Soni, R. K.; Quadri, L. E. N.*; Tan, D. S.* J. Am. Chem. Soc. 2007, 129, 7752–7753.
    Abstract | PubMed | PMC ]
    Journal of the American Chemical Society 2007 graphical abstract

    (Highlighted in Faculty of 1000 Biology )

  29. A unified synthetic approach to polyketides having both skeletal and stereochemical diversity.
    Shang, S.; Iwadare, H.; Macks, D. E.; Ambrosini, L. M.; Tan, D. S.* Org. Lett. 2007, 9, 1895–1898.
    Abstract | PubMed | PMC ]
    Organic Letters 2007 graphical abstract

  30. Stereocontrolled synthesis of spiroketals via Ti(Oi-Pr)4-mediated kinetic spirocyclization of glycal epoxides with retention of configuration.
    Moilanen, S. B.; Potuzak, J. S.; Tan, D. S.* J. Am. Chem. Soc. 2006, 128, 1792–1793.
    Abstract | PubMed | PMC ]
    Jounral of the American Chemical Society 2006 graphical abstract

    (Highlighted in Nature )

  31. Stereocontrolled synthesis of spiroketals via a remarkable methanol-induced kinetic spirocyclization reaction.
    Potuzak, J. S.; Moilanen, S. B.; Tan, D. S.* J. Am. Chem. Soc. 2005, 127, 13796–13797.
    Abstract | PubMed  ]
    Journal of the American Chemical Society 2005 graphical abstract

  32. Diversity-oriented synthesis: Exploring the intersections between chemistry and biology.
    Tan, D. S.* Nat. Chem. Biol. 2005, 1, 74–84.
    Abstract | PubMed ]
    Nature Chemical Biology 2005 graphical abstract

  33. Small-molecule inhibition of siderophore biosynthesis in Mycobacterium tuberculosis and Yersinia pestis.
    Ferreras, J. A.; Ryu, J.-S.; Di Lello, F.; Tan, D. S.*, Quadri, L. E. N.* Nat. Chem. Biol. 2005, 1, 29–32.
    Abstract | PubMed ]
    Nature Chemical Biology 2005 graphical abstract

    (Highlighted in Nature, Nat. Chem. Biol., Chem. Eng. News., and Mercosur Económico )

  34. Advancing chemistry and biology through diversity-oriented synthesis of natural product-like libraries.
    Shang, S.; Tan, D. S.* Curr. Opin. Chem. Biol. 2005, 9, 248–258.
    Abstract | PubMed ]
    Current Opinion in Chemical Biology 2005 graphical abstract

  35. An acid-stable tert-butyldiarylsilyl (TBDAS) linker for solid-phase organic synthesis.
    DiBlasi, C. M.; Macks, D. E.; Tan, D. S.* Org. Lett. 2005, 7, 1777–1780.
    Abstract | PubMed ]
    Organic Letters 2005 graphical abstract

    (Highlighted in Lett. Org. Chem. [PDF] )

  36. Enantioselective synthesis of erythro-4-deoxyglycals as scaffolds for target- and diversity-oriented synthesis: New insights into glycal reactivity.
    Moilanen, S. B.; Tan, D. S.* Org. Biomol. Chem. 2005, 3, 798–803.
    Abstract | PubMed ]
    Organic and Biomolecular Chemistry 2005 graphical abstract

  37. Current progress in natural product-like libraries for discovery screening.
    Tan, D. S.* Comb. Chem. High-Throughput Screen. 2004, 7, 631–643.
    Abstract | PubMed ]
    Combinatorial Chemistry and High-Throughput Screening 2004 graphical abstract

  38. Synthesis of C1-alkyl and C1-acylglycals from glycals using a B-alkyl Suzuki–Miyaura cross coupling approach.
    Potuzak, J. S.; Tan, D. S.* Tetrahedron Lett. 2004, 45, 1797–1801.
    Abstract ]
    Tetrahedron Letters 2004 graphical abstract

  39. Discovery and applications of small molecule probes for studying biological processes.
    Potuzak, J. S.; Moilanen, S. B.; Tan, D. S.* Biotechnol. Genet. Eng. Rev. 2004, 21, 11–78.
    TOC | PDF | PubMed ]
    Biotechnology and Genetic Engineering Reviews 2004 graphical abstract

  40. Sweet surrender to chemical genetics.
    Tan, D. S.* Nat. Biotechnol. 2002, 20, 561–563.
    Abstract | PubMed ]
    Nature Biotechnology 2002 graphical abstract


Postdoctoral Publications

  1. Total synthesis of guanacastepene A: A route to enantiomeric control.
    Mandal, M.; Yun, H.; Dudley, G. B.; Lin, S.; Tan, D. S.; Danishefsky, S. J.* J. Org. Chem. 2005, 70, 10619–10637.
    Abstract | PubMed ]
    Journal of Organic Chemistry 2005 graphical abstract

    (Featured on the Cover )

  2. Synthesis of the functionalized tricyclic skeleton of guanacastepene A: A tandem epoxide-opening β-elimination/Knoevenagel cyclization.
    Tan, D. S.; Dudley, G. B; Danishefsky, S. J.* Angew. Chem., Int. Ed. 2002, 41, 2185–2188.
    Abstract | PubMed ]
    JOURNAL YEAR graphical abstract

  3. A stereoselective route to guanacastepene A through a surprising epoxidation.
    Lin, S.; Dudley, G. B.; Tan, D. S.; Danishefsky, S. J.* Angew. Chem., Int. Ed. 2002, 41, 2188–2191.
    Abstract | PubMed ]
    JOURNAL YEAR graphical abstract

  4. Remarkable stereoselectivity in the alkylation of a hydroazulenone: Progress toward the total synthesis of guanacastepene.
    Dudley, G. B.; Tan, D. S.; Kim, G.; Tanski, J. M.; Danishefsky, S. J.* Tetrahedron Lett. 2001, 42, 6789–6791.
    Abstract ]
    Tetrahedron Letters 2001 graphical abstract


Graduate Publications

  1. A mercury-catalyzed transetherification cyclization leading to fused cyclic polyethers.
    Tan, D. S.; Schreiber, S. L.* Tetrahedron Lett. 2000, 41, 9509–9513.
    Abstract ]
    Tetrahedron Letters 2000 graphical abstract

  2. Ligand discovery using encoded combinatorial libraries.
    Tan, D. S.*; Burbaum, J. J.* Curr. Opin. Drug Discovery Dev. 2000, 3, 439–453.
    Abstract | PubMed ]
    Current Opinion in Drug Discovery 2000 graphical abstract

  3. Synthesis and preliminary evaluation of a library of polycyclic small molecules for use in chemical genetic assays.
    Tan, D. S.; Foley, M. A.; Stockwell, B. R.; Shair, M. D.; Schreiber, S. L.* J. Am. Chem. Soc. 1999, 121, 9073–9087.
    Abstract ]
    Journal of the American Chemical Society 1999 graphical abstract

  4. Stereoselective synthesis of over two million compounds having structural features both reminiscent of natural products and compatible with miniaturized cell-based assays.
    Tan, D. S.; Foley, M. A.; Shair, M. D.; Schreiber, S. L.* J. Am. Chem. Soc. 1998, 120, 8565–8566.
    Abstract ]
    Journal of the American Chemical Society 1998 graphical abstract

    (Highlighted in Science, Chem. Eng. News. )


Undergraduate Publication

  1. Enzymatic resolution coupled with substrate racemization using a thioester substrate.
    Tan, D. S.; Günter, M. M.; Drueckhammer, D. G.* J. Am. Chem. Soc. 1995, 117, 9093–9094.
    Abstract ]
    Journal of the American Chemical Society1995 graphical abstract