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Robert W. Huigens III, Ph.D.

Robert W. Huigens III

Assistant Professor

Medicinal Chemistry

OFFICE: UF Health Science Center, Medical Science Bldg,1345 Center Drive, Room P5-33

EMAIL: rwhuigens@ufl.edu

PHONE: (352) 273-7718

CV: Link to CV

 

Education

  • B.A. Biology, University of North Carolina at Greensboro, 2000-2003
  • Ph.D. Chemistry, North Carolina State University, 2004-2009
  • American Cancer Society Postdoctoral Fellow, University of Illinois at Urbana-Champaign, 2009-2013

Biographical Sketch

Robert W. Huigens III received his bachelors in biology from the University of North Carolina at Greensboro in 2003 where he first developed an interest in organic synthesis and medicine.  He went on to pursue his graduate studies in organic chemistry at North Carolina State University under the direction of Christian Melander. During his time at North Carolina State University, Dr. Huigens started the biofilm program in the Melander lab while evaluating the biofilm inhibition and dispersal activity of several libraries of ageliferin-inspired small molecules he had synthesized. In 2009, he completed his Ph.D. in chemistry and went on to become an American Cancer Society postdoctoral fellow at the University of Illinois at Urbana-Champaign under the guidance of Paul Hergenrother. As a postdoctoral fellow in the Hergenrother lab, Dr. Huigens developed a rapid approach to generate complex and diverse small molecules from commercially available natural products using various ring-distortion reactions for high-throughput screens in drug discovery efforts (i.e., “Complexity-to-Diversity”).

In 2013, Dr. Huigens joined the Medicinal Chemistry Department at the University of Florida College of Pharmacy as an assistant professor. His research interests include organic synthesis, drug discovery, medicinal chemistry, chemical biology, antibacterial agents and personalized cancer therapeutics. Recently, Dr. Huigens was the recipient of two Young Investigator Awards from the American Chemical Society (Division of Medicinal Chemistry) and the Center for Biofilm Engineering (Montana State University) for his group’s discovery of novel and potent bacterial biofilm-eradicating agents.

Research Interests

The overarching goal of the Huigens lab is to push back the boundaries of drug discovery using new and innovative strategies to tackle unmet challenges associated with complex molecule synthesis, drug-resistant bacteria and cancer. Students and postdocs in our group receive training at the interface of chemistry and biology using a combination of synthetic organic chemistry, medicinal chemistry, chemical biology and microbiology approaches. We currently have three major areas of research (click on the link below for more on our research programs):

Huigens Group Members

Professor Robert W. Huigens III – Principal Investigator
Nicholas Paciaroni – Graduate Student (B.S. Chemistry; Clemson University)
Aaron Garrison – Graduate Student (B.A. Biochemistry; University of South Florida)
Yasmeen Abouelhassan – Graduate Student (B.S. Pharmacy; Cairo University)
Akash Basak – Chemistry Graduate Student (M.S. Chemistry; ITT Kanpur)
Chip Norwood – Graduate Student (B.S. Chemistry; East Tennessee State University)
Hongfen Yang – Graduate Student (M.S. Chemistry; Chinese Academy of Sciences)
Gena Burch – PharmD/PhD Student (B.S. Chemistry; Hillsdale College)
Hussain Yousaf – Undergraduate Researcher (Biologist)
Will Wang – High School Researcher (SSTP summer student)
Austin Arnold – Undergraduate Researcher (Chemistry Major)

University of Florida Affiliations

  1. Chemistry Department (courtesy faculty appointment)
  2. Center for Natural Products, Drug Discovery and Development (CNPD3)
  3. Emerging Pathogens Institute (EPI)
  4. UF Health Cancer Center

Huigens Lab Publications

  • Zuo R.; Garrison A.T.; Basak A.; Zhang P.; Huigens III, R. W.; Ding Y. “In vitro antifungal and antibiofilm activities of halogenated quinoline analogues against Candida albicans and Cryptococcus neoformans.” In press, Int. J. Antimicrob. Agents.
  • Basak, A.; Abouelhassan, Y.; Norwood IV, V. M.; Bai, F.; Nguyen, M.; Jin, S.; Huigens III, R. W. “Synthetically Tuning the 2-Position of Halogenated Quinolines: Optimizing Antibacterial and Biofilm Eradication Activities via Alkylation and Reductive Amination Pathways.” Chem. Eur. J. 2016, 22, 9181-9189. Hot Paper, Cover Art Selection, Highlighted in Angew. Chemie. Int. Ed.
  • Garrison, A. T.; Abouelhassan, Y.; Norwood IV, V. M.; Kallifidas, D.; Bai, F.; Nguyen, M.; Rolfe, M. Burch, G. M., Jin, S., Luesch, H.; Huigens III, R. W. “Structure-Activity Relationships of a Diverse Class of Halogenated Phenazines that Targets Persistent, Antibiotic-Tolerant Bacterial Biofilms and Mycobacterium tuberculosis.” J. Med. Chem. 2016, 59, 3808-3825.
  • Paciaroni, N. G.; Borrero, N. V.; Rocca, J. R., Huigens III, R. W. “Rapid Synthesis of Phenazine-1-Carboxyilc Acid Derived Small Molecules from Diverse Anilines: Privileged Structures for Discovery.” Research & Reviews: Journal of Medicinal & Organic Chemistry, 2015, 2, 67-76.
  • Garrison, A. T.; Abouelhassan, Y.; Kallifidas, D.; Bai, F.; Ukhanova, M.; Mai, V.; Jin, S.; Luesch, H.; Huigens III, R. W. “Halogenated Phenazines that Potently Eradicate Biofilms, MRSA Persister Cells in Non-Biofilm Cultures and Mycobacterium tuberculosis.” Angew. Chemie Int. Ed., 2015, 54, 14819-14823.
  • Basak, A.; Abouelhassan, Y.; Huigens III, R. W. “Halogenated Quinolines Discovered Through Reductive Amination with Potent Eradication Activities against MRSA, MRSE and VRE Biofilms.” Org. Biomol. Chem., 2015, 13, 10290-10294. 2015 Hot Articles in Organic and Biomolecular Chemistry
  • Abouelhassan, Y.; Garrison, A. T.; Bai, F.; Norwood IV, V. M.; Nguyen, M.; Jin, S.; Huigens III, R. W. “A Phytochemical-Halogenated Quinoline Combination Therapy Strategy for the Treatment of Pathogenic Bacteria” ChemMedChem, 2015, 10, 1157-1162.
  • Garrison, A. T.; Bai, F.; Abouelhassan, Y.; Paciaroni, N. G.; Jin, S.; Huigens III, R.W. “Bromophenazine Derivatives with Potent Inhibition, Dispersion and Eradication Activities against Staphylococcus aureus Biofilms.” RSC Adv. 2015, 5, 1120-1124.
  •  Abouelhassan, Y.; Garrison, A. T.; Burch, G. M.; Wong, W.; Norwood IV, V. M.; Huigens III, R. W. “Discovery of quinoline small molecules with potent dispersal activity against methicillin-resistant Staphylococcus aureus and Staphylococcus epidermidis biofilms using a scaffold hopping strategy.” Bioorg. Med. Chem. Lett., 2014, 24, 5076-5080.
  •  Borrero, N.V.; Bai, F.; Perez, C.; Duong, B.Q.; Rocca, J.R.; Jin, S.; Huigens III, R.W. “Phenazine antibiotic inspired discovery of potent bromophenazine antibacterial agents against Staphylococcus aureus and Staphylococcus epidermidis.” Org. Biomol. Chem. 2014, 12, 881-886.

Select Publications from Graduate and Postdoctoral Studies

  • Huigens III, R.W.; Morrison, K.C.; Hicklin, R.W.; Flood Jr., T.A.; Richter, M.F.; Hergenrother, P.J. “A ring-distortion strategy to construct stereochemically complex and structurally diverse compounds from natural products.” Nature Chem. 2013, 5, 195-202.
  • Rogers, S.A.; Huigens III, R.W.; Cavanagh, J.; Melander, C. “Synergistic effects between conventional antibiotics and 2-aminoimidazole-derived antibiofilm agents.” Antimicrob. Agents & Chemother. 2010, 54, 2112-2118.
  • Huigens III, R.W.; Reyes, S.; Reed, C. S.; Bunders, C.; Rogers, S.A.; Steinhauer, A.T.; Melander, C. “The chemical synthesis and antibiotic activity of a diverse library of 2-aminobenzimidazole small molecules against MRSA and multidrug-resistant A. baumannii.” Bioorg. & Med. Chem. 2010, 18, 663-674.
  • Rogers, S.A.; Huigens III, R.W.; Melander, C. “A 2-aminobenzimidazole that inhibits and disperses gram-positive biofilms through a zinc-dependent mechanism.” J. Am. Chem. Soc. 2009, 131, 9868-9869.
  • Huigens III, R.W.; Rogers, S.A., Steinhauer, A.T., and Melander, C. “Inhibition of Acinetobacter baumannii, Staphylococcus aureus, and Pseudomonas aeruginosa biofilms with a class of TAGE-triazole conjugates.” Org. Biomolec. Chem. 2009, 7, 794-802.
  • Huigens III, R.W.; Ma, L.; Gambino, C.; Moeller, P.D.R.; Basso, A.; Cavanagh, J.; Wozniack, D.J.; Melander, C. “Control of bacterial biofilms with marine alkaloid derivatives.” Mol. BioSys. 2008, 4, 614-621.
  • Huigens III, R.W.; Richards J.J.; Parise, G.; Ballard, T.E.; Zeng, W.; Deora, R.; Melander, C. “Inhibition of Pseudomonas aeruginosa biofilm formation with bromoageliferin analogues.”  J. Am. Chem. Soc. 2007, 129, 6966-6967.

Highlighted Publications and Other Press