Medicinal Chemistry

Faculty

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Kerwin, Sean M., Ph.D.
Professor of Med. Chem.
G.D. Searle & Co.
Endowed Fellowship in Pharmacy
BME 6.202C
512-471-5074
skerwin@austin.utexas.edu


Selected Publications

  • Plyler, J.; Jasheway, K.; Karr, J.; Brennan, J. S.; Kerwin, S. M.; David, W. M. “Real-time Investigation of SV40 Large T-antigen Helicase Activity Using Surface Plasmon Resonance” Cell Biochem. Biophys. 2009, 53, 43-52.
  • Galal, S. A.; Hagab, K. H.; Kassab, A. S.; Rodriguez, M.; Kerwin, S. M.; El-Khamry, A-M. A.; El Diwani, H. I. “New Transition Metal Ion Complexes with Benzimidazole-5-Carboxylic Acid Hydrazides with Antitumor Activity” Eur. J. Med. Chem., 2009, 44, 1500-1508.
  • Marriner, W. A.; Kerwin, S. M. “An Improved Synthesis of N’-Nitroso-Nornicotine-5’-Acetate” J. Org. Chem. 200974,  2891-2892.
  • Laroche, C.; Li, J.; Kerwin, S. M. “Lithiation and Functionalization of N-Alkynylimidazoles at the 2-Position” Tetrahedron Lett. 2009, 50, 5194-5197.
  • Wang, X.; Pang, J.; Maffucci, J. A.; Newman, R. A.; Kerwin, S. M.; Bowman, P. D.; Stavchansky, S.  “Pharmacokinetics of Caffeic Acid Phenethyl Ester and its Catechol-Ring Fluorinated Derivative Following Intravenous Administration to Rats”  Biopharm. Drug Disp. 2009, 30, 221-228.
  • Laroche, C.; Kerwin, S. M. “Efficient, Regioselective Access to Bicyclic Imidazo[1,2-x]- Heterocycles via Gold and Base Promoted Cyclization of 1-Alkynylimidazoles” J. Org. Chem. 2009, 74, 9229-9232.
  • Li, J.; Kaoud, T. S.; Laroche, C.; Dalby, K. N.; Kerwin, S. M. “Synthesis and Biological Evaluation of p53a Kinase-Targeting Dialkynylimidazoles.” Bioorg. Med. Chem. Lett.  2009, 19, 6293-6297.
  • Wang, X.; Stavchansky, S.; Kerwin, S. M.; Bowman, P. D. “Structure-activity Relationships in the Cytoprotective Effect of Caffeic Acid Phenethyl Ester (CAPE) and Fluorinated Derivatives: Effects on Heme Oxygenase-1 Induction and Antioxidant Activities. Eur. J. Pharmacol. 2010, 635, 16-22.
  • Laroche, C.; Li, J.; Golzales, C.; David, W. M.; Kerwin, S. M. “Cyclization Kinetics and Biological Evaluation of an Anticancer 1,2-Dialkynylimidazole” Org. Biomol. Chem. 2010, 8, 1535 – 1539.
  • Yang, J.; Marriner, G. A.; Wang, X.; Bowman, P. D.; Kerwin, S. M.; Stavchansky, S. “Synthesis of a Series of Caffeic Acid Phenethyl Amide (CAPE) Fluorinated Derivatives: Comparison of Cytoprotective Effects to Caffeic Acid Phenethyl Ester (CAPE)” Bioorg. Med. Chem. 2010, 18, 5032-5038.
  • Laroche, C.; Li, J.; Kerwin, S. M. “Cytotoxic 1,2-Dialkynylimidazole-Based Aza-Enediynes:  Aza-Bergman Rearrangement Rates do not Predict Cytotoxicity” J. Med. Chem. 2011, 54, 5059-5069.
  • Yang, J.; Kerwin, S. M.; Bowman, P. P., Stavchansky, S. “Stability of Caffeic Acid Phenethyl Amide (CAPA) in Rat Plasma" Biomed. Chromatogr. 2012, 26, 594-598.
  • Schoonover, M.; Kerwin, S. M.“G-Quadruplex DNA Cleavage Preference and Identification of a Perylene Diimide G-Quadruplex Photocleavage Agent Using a Rapid Fluorescent Assay”  Bioorg. Med. Chem. 2012, 20, 6904–6918.
  • Omar, M. A.; Shaker, Y. M.; Galal, S. A.; Ali, M. M. Kerwin, S. M.; Li, J.; Tokuda, H.; Ramadan, R. A. El Diwani, H. I. “Synthesis and docking studies of novel antitumor benzimidazoles” Bioorg. Med. Chem. 2012, 20, 6989–7001.
  • Li, J.; Kaoud, T. S.; LeVieux, J.; Gilbreath, B.; Moharana, S.; Dalby, K, N.; Kerwin, S. M. “A fluorescence-based assay for p38a docking site binders: Identification of the Hypoxis natural product rooperol as a novel p38a kinase inhibitor” ChemBioChem, 2013, 14, 66–71.
  • Kerwin, S. M.; Cha, J. “A concise synthesis of rooperol and related 1,5-diarylpent-1-en-4-ynes” Tetrahedron Lett. 2014, 55, 137-141.
  • Yang, J.; Bowman, P. D.; Kerwin, S. M.; Stavchansky, S. “Development and validation of an LCMS method to determine the pharmacokinetic profiles of caffeic acid phenethyl amide and caffeic acid phenethyl ester in Sprague-Dawley rats” Biomed. Chromatogr. 2014, 28, 241-246.
  • Laroche, C.; Gilbreath, B.; Kerwin, S. M. “Exploring the synthetic utility of 1-alkynylimidazoles:  Regiocontrolled cyclization to diverse imidazoazines and imidazoazoles” Tetrahedron 2014 70, 4534-4539.
More information about Dr. Kerwin
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> Kerwin Lab Pages
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Last Reviewed: January 28, 2015

Division Information

Mailing Address:
The University of Texas
at Austin
Medicinal Chemistry
BME 6.202
College of Pharmacy
The University of Texas
at Austin
2409 University Ave.
Stop A1900
Austin, TX, USA
78712-1113

Email Address: pharmacy
@austin.utexas.edu

Phone: 512-471-5263
Fax: 512-232-2606


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