31. Enantioselective Tandem Cyclization of Alkyne-Tethered Indoles Using Cooperative Silver(I) and Chiral Phosphoric Acid Catalysis. Zhu Y, He W, Wang W, Pitsch CE, Wang X, Wang X, Angew Chem, accepted.

DOI: 10.1002/anie.201706694 and 10.1002/ange.201706694 [link]

Asymmetric catalysis

30.  Diastereoselective Synthesis and Biological Evaluation of Enantiomerically Pure Tricyclic Indolines. He W, Griffiths BM, Wang W, Wang X, Org. Biomol. Chem., 2017;15:4241-4245.

DOI: 10.1039/C7OB00897J [link]

Diastereoselective synthesis of tricyclic indolines

29. Tetracyclic Indolines as a Novel Class of β-Lactam-Selective Resistance Modifying Agent for MRSA. Zhu Y, Cleaver L, Wang W, Podoll JD, Walls S, Jolly A, Wang X. Eur J Med Chem. 2017;125:130-142.

DOI: 10.1016/j.ejmech.2016.09.034 [link]

tetracyclic indoline

28. Bioinspired Discovery of Chemical Reactions and Biological Probes. Griffiths B, Burl J, Wang X. Synlett. 2016;27:2039-2042.

DOI: 10.1055/s-0035-1561638 [link]

bioinspired discovery

27. Property-Guided Synthesis of Aza-Tricyclic Indolines: Development of Gold Catalysis En Route. Barbour PM, Wang W, Chang L, Pickard KL, Rais R, Slusher BS, Wang X. Adv Synth Catal. 2016;358:1482-1490. [Theme: Gold Catalysis: Quo Vadis?]

DOI: 10.1002/adsc.201501101 [link]

aza-tricyclic indoline

26. A Fluorescence Polarization Biophysical Assay for the Naegleria DNA Hydroxylase Tet1. Marholz LJ, Wang W, Zheng Y, Wang X. ACS Med Chem Lett. 2016;7:167-171. [Theme: Epigenetics] 

DOI: 10.1021/acsmedchemlett.5b00366 [link]

Graph 1

25. Gold-Catalyzed Cyclization Leads to A Bridged Tetracyclic Indolenine That Represses β-Lactam Resistance. Xu W, Wang W, Wang X. Angew Chem Int Ed. 2015;54:9546-9549; Angew Chem. 2015;127:9682-9685.

DOI: 10.1002/anie.201503736 (International) and 10.1002/ange.201503736 (German) [link]


24. Novel Scaffolds of Cell-Active Histone Demethylase Inhibitors Identified from High-Throughput Screening. Wang W, Marholz LJ, Wang X. J Biomol Screen. 2015;20:821-827

DOI: 10.1177/1087057115579637 [link]; Featured on GMD [link]

Graph 2

23. Discovery and Initial Structure-Activity Relationships of N-Benzyl Tricyclic Indolines as Antibacterials for Methicillin-Resistant Staphylococcus Aureus. Barbour PM, Podoll JD, Marholz LJ, Wang X. Bioorg Med Chem Lett. 2014;24:5602-5605.  

DOI: 10.1016/j.bmcl.2014.10.094. [link

Graph 3

22. Development of Substrate-Selective Probes for Affinity Pulldown of Histone Demethylases. Marholz LJ, Chang L, Old WM, Wang X. ACS Chem Biol. 2015;10:129-137.

DOI: 10.1021/cb5006867 [link]

Graphical abstract

21. A Histone Demethylase Inhibitor, Methylstat, Inhibits Angiogenesis in vitro and in vivo. Cho Y, Kim KH, Xu W, Wang X, Kwon HJ. RSC Adv. 2014;4:38230-38233.

DOI: 10.1039/c4ra07154a [link]


20. Structure-Activity Relationship Studies of the Tricyclic Indoline Resistance-Modifying Agent. Chang L, Podoll JD, Wang W, Walls S, O'Rourke CP, Wang X. J Med Chem. 2014;57:3803-3817

DOI: 10.1021/jm500146g [link]

Graph 4

19. Gold Approaches to Polycyclic Indole Alkaloids. Barbour PM, Marholz LJ, Chang L, Xu W, Wang X. Chem Lett. 2014;43:572-578

DOI: 10.1246/cl.131230 [link]

Gold catalysis

18. Bio-Inspired Synthesis Yields A Tricyclic Indoline That Selectively Resensitizes MRSA to β-Lactam Antibiotics. Podoll JD, Liu Y, Chang L, Walls S, Wang W, Wang X. Proc Natl Acad Sci USA. 2013;110:15573-15578. 

DOI: 10.1073/pnas.1310459110 [link]; Highlighted by PNAS [link]; Recommended by Faculty of 1000 [link]

Bio-inspired synthesis

17. Quantitative Analysis of Histone Demethylase Probes Using Fluorescence Polarization. Xu W, Podoll JD, Dong X, Tumber A, Oppermann U, Wang X. J Med Chem.  2013;56:5198-5202. 

DOI: 10.1021/jm3018628 [link]; Highlighted by Nature SciBX [link]

Graph 5

16. A One-Pot Three-Component Reaction for the Preparation of Highly Functionalized Tryptamines. Yeo SJ, Liu Y, Wang X. Tetrahedron2012;68:813-818. 

DOI: 10.1016/j.tet.2011.11.032 [link]


15. A Selective Inhibitor and Probe of the Cellular Functions of Jumonji C Domain-Containing Histone Demethylases. Luo X, Liu Y, Kubicek S, Myllyharju J, Tumber A, Ng S, Che KH, Podoll J, Heightman TD, Oppermann U, Schreiber SL, Wang X. J Am Chem Soc. 2011;133:9451-9456. 

DOI: 10.1021/ja201597b [link]; Highlighted by Nature SciBX [link]

Graph 6

14. Selective Gold(I)-Catalyzed Formation of Tetracyclic Indolines: A Single Transition State and Bifurcations Lead to Multiple Products. Noey EL, Wang X, Houk KN. J Org Chem. 2011;76:3477-83. 

DOI: 10.1021/jo200556f [link]

Graph 7

13. Gold(I)-Catalyzed Tandem Cyclization Approach to Tetracyclic Indolines. Liu Y, Xu W, Wang X. Org Lett. 2010;12:1448-51. 

DOI: 10.1021/ol100153h [link]

Gold catalysis graph

12. AAK1 Identified as an Inhibitor of Neuregulin-1/ErbB4-Dependent Neurotrophic Factor Signaling Using Integrative Chemical Genomics and Proteomics. Kuai L, Ong SE, Madison JM, Wang X, Duvall JR, Lewis TA, Luce CJ, Conner SD, Pearlman DA, Wood JL, Schreiber SL, Carr SA, Scolnick EM, Haggarty SJ. Chem & Biol. 2011;18;891-906. [link]

11. Chemical genetics identifies small-molecule modulators of neuritogenesis involving neuregulin-1/ErbB4 signaling. Kuai L, Wang X, Madison JM, Schreiber SL, Scolnick EM, Haggarty SJ. ACS Chem Neurosci. 2010;1;325-42. [link]

10. Syntheses of aminoalcohol-derived macrocycles leading to a small-molecule binder to and inhibitor of sonic hedgehog. Peng LF, Stanton BZ, Maloof N, Wang X, Schreiber SL. Bioorg Med Chem Lett. 2009;19: 6319-25. [link]

9. Identifying the proteins to which small-molecule probes and drugs bind in cells. Ong SE, Schenone M, Margolin AA, Li X, Do K, Doud MK, Mani DR, Kuai L, Wang X, Wood JL, Tolliday NJ, Koehler AN, Marcaurelle LA, Golub TR, Gould RJ, Schreiber SL, Carr SA. Proc Natl Acad Sci U S A. 2009;106;4617-22. [link]

8. A small molecule that binds Hedgehog and blocks its signaling in human cells. Stanton B, Peng LF, Maloof N, Nakai K, Wang X, Duffner JL, Taveras KM, Hyman JM, Lee SW, Koehler AN, Chen JK, Fox JL, Mandinova A, Schreiber SL. Nat Chem Biol. 2009;5:154-6. [link] 

7. Diversity synthesis of complex pyridines yields a probe of a neurotrophic signalling pathway. Gray BL, Wang X, Brown WC, Kuai L, Schreiber SL. Org Lett. 2008;10:2621-4. [link]

6. Small-molecule reagents for cellular pull-down experiments. Wang X, Imber BS, Schreiber SL. Bioconjug Chem. 2008;19:585-7. [link]

5. Synthesis of the tetracyclic core of the tetrapetalones via transannular oxidative [4+3] cyclization. Wang X, Porco JA Jr. Angew Chem Int Ed Eng. 2005;44:3067-71; Corrigendum: 2006;45:6607. [link]

4. Total synthesis of the salicylate enamide macrolide oximidine III: application of relay ring-closing metathesis. Wang X, Bowman EJ, Bowman BJ, Porco JA Jr. Angew Chem Int Ed Eng. 2004;43:3601-5. [link]

3. Total synthesis of the salicylate enamide macrolide oximidine II. Wang X, Porco JA Jr. J Am Chem Soc. 2003;125:6040-1. [link]

2. Modification of C-terminal peptides to form peptide enamides: synthesis of chondriamides A and C. Wang X, Porco JA Jr. J Org Chem. 2001;66:8215-21. [link]

1. Parallel synthesis and purification using anthracene-tagged substrates. Wang X, Parlow JJ, Porco JA Jr. Org Lett. 2000;2:3509-12. [link]

1.Histone demethylase inhibitors and methods for using the same. Wang X, Xu W. U.S. 8,735,622 [link] licensed by Millipore [link] and Sigma-Aldrich [link]

2. “Indoline Alkaloid Compounds,” Podoll JD; Chang L; Wang X. PCT/US14/32585.

3. "Polycycilc Indoline and Indolenine Compounds," Barbour PM, Wang X PCT/US62/154,792.