A significant, current challenge in chemical biology and drug discovery is to identify small molecule probes and therapeutic lead compounds to address novel biological targets. We are engaged in a two-pronged approach to this problem involving diversity-oriented synthesis and rational design as complementary approaches to ligand discovery. At the core of these efforts is the development of new synthetic methodologies to provide flexible, efficient, systematic access to these structures. We leverage multidisciplinary collaborations with biologists to evaluate the molecules we synthesize with the long-term goals of probing key biological processes and exploring new therapeutic opportunities in cancer and infectious diseases.


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 ]

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 ]
(Highlighted in SciBX )

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 ]

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

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

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Selected Achievements

Development of salicyl-AMS, a novel antibacterial agent to treat tuberculosis and other infections

Louise and Allston Boyer Young Investigator Award for Basic Research, Memorial Sloan Kettering Cancer Center (2010)

Dean's Award for Excellence in Teaching and Mentoring, Weill Cornell Graduate School of Medical Sciences (2013)

Derek Tan

At Work: Chemist Derek Tan

Chemist Derek Tan creates small molecules to probe biological processes and investigate new therapeutic targets for cancer.