Bioorganic and Medicinal Chemistry
We are interested in using chemistry to understand biological processes. Central to our theme is organic chemistry as a tool that intersects with molecular life sciences such as molecular and cell biology. Our primary focus is the development of chemical toolboxes to address problems in biology. Currently, our work is aimed at the following:
- Development of novel diboron reagents for the mild and selective boration of activated carbon-carbon bonds
- Development of medium-sized branched peptides to target RNA structures associated with HIV as the next generation anti-HIV therapeutics
- Defining the roles of sphingosine kinases in hyperproliferative diseases by developing cell permeable small molecule libraries as probes
- Development of N-terminal peptidic boronic acids as protease inhibitors
- Peck, C.L.; Calderone, J.A. and Santos, W.L. Copper(II)-catalyzed beta-Borylation of Acetylenic Esters in Water. Synthesis, 2015, in press. DOI: 10.1055/s-0034-1380524.
- Guo, X.; Nelson, A.K.; Slebodnick, C. and Santos, W.L. Regio- and Chemoselective Diboration of Allenes with Unsymmetrical Diboron: Formation of Vinyl and Allyl Boronic Acid Derivatives, ACS Catal., 2015, 5, 2172-2176.DOI: 10.1021/acscatal.5b00387.
- Patwardhan, N.N.; Morris, E.A.; Raje, M.R.; Gao, M.; Kharel, Y.; Tomsig, J.L.; Lynch, K.R. and Santos, W.L. "Structure-Activity Relationship Studies and In Vivo Activity of Guanidine-based Sphingosine Kinase Inhibitors: Discovery of SphK 1 and 2 Selective Inhibitors." J. Med. Chem. 2015, 58, 1879-1899. DOI: 10.1021/jm501760d.
- Santos, W.L. and Lynch, K.R. Drugging Sphingosine Kinases. ACS Chem. Biol. 2015, 10, 225-223.DOI:10.1021/cb5008426
- Calderone, J.A. and Santos, W.L. Copper(II)-Catalyzed Silylation of Activated Alkynes in Water: Diastereodivergent Access to (E)- or (Z)- beta-Silyl-alpha, beta-Unsaturated Carbonyl and Carboxyl Compounds. Angew. Chem. Int. Ed. 2014, 53, 4154-4158. DOI: 10.1002/anie.201310695
- Cliff and Agnes Lilly Faculty Fellow of Drug Discovery, 2015, 2017
- Innovators Award, Virginia Tech, 2014
- John C. Schug Research Award, 2014
- ACS Young Academic Investigator, Philadelphia, PA, 2012
- Molecular Biosystems Award Symposium, 2011
- Co-founder, SphynKx Therapeutics, 2010
- Chemical Communications Emerging Investigator, 2010
- Blackwood Junior Faculty Fellow of Life Sciences, 2010–present
- Molecular BioSystems Emerging Investigator, 2009
- Ruth Kirstein NRSA Fellow, 2003–2006
- B.S. University of Virginia, 1997
- Ph.D. University of Virginia, 2002
- NIH Postdoctoral Fellow, Harvard University, 2002–2006