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Moulder Center for Drug Discovery Research



Selected Publications

Dr. Magid Abou-Gharbia

  1. "ILS-900, a novel, non-immunosuppressive rapamycin analog, promotes sustained functional recovery following cerebral ischemia", A. Wood, S. Liang, Y. Chen D. Liu, C. Gonzales, M. L. Mercado, K. Pong, Z. Cao, E. I. Graziani, M. Abou-Gharbia,P.H. Reinhart, M. N. Pangalosand, M. M. Zaleska, PANAS, in press.
  2. "Begacestat (GSI-953): A Novel, Selective Thiophene Sulfonamide Inhibitor of Amyloid Precursor Protein - Secretase for the Treatment of Alzheimer's Disease", R. L. Martone, H. Zhou, K. Atchison, T. Comery, J. Z. Xu, X. Huang, X. Gong, M. Jin, A. Kreft, B. Harrison, S. C. Mayer, S. Aschmies, C. Gonzales, M. M. Zaleska, D. R. Riddell, E. Wagner, P. Lu, S. C. Sun, J. Sonnenber-Reines, A. Oganesian, K. Adkins, M. Leach, D. W. Clarke, D. Huryn, M. Abou-Gharbia, R. Magdola, J. Bard, G. Frick, S. Raje, S. B. Forlow, C. Balliet, M. E. Burczynski, J. Pharm. Exp. Ther., in press. 331(2), 598-608(2009).
  3. "Comparison of Human and Rat Uterine Leiomyomata: Identification of a Dysregulated mTOR Pathway", J. S. Crabtree, S. A. Jelinsky, H. A. Harris, S. E. Choe, M. M. Cotreau, M. L. Kimberland, E. Wilson, K. A. Saraf, W. Liu, A. S. McCampbell, B. Dave, R. R. Broadus, E. L. Brown, W. Kao, J. S. Stotnicki, M. Abou-Gharbia, R. C. Winneker, and C. L. Walker, Cancer Research, 69 (15):6171-8 (2009).
  4. "Discovery of Innovative Small molecule Therapeutics" Magid Abou-Gharbia, J.Med.Chem, 52:1, 2-9 (2009).
  5. "Prodrugs of Perzinfotel with Improved Oral Bioavailability" R.B.Baudy, J.A. Butera, M.Abou-Gharbia, H.Chen, B. Harrison, U. Jain, R.Magolda, J.Y.Sze, M.R.Brandt, T.A.Cummons, D.Kowal, M.N.Pangalos, B.Zupan, M. Hoffmann, M.May, C.Mugford, J.Kennedy, and W.Childers Jr., J.Med.Chem , 52:3, 771-8 (2009)
  6. "Discovery of Begacestat, a notch-1-Sparing gamma Secretase Inhibitor for the treatment of Alzheimer's Disease, " S. C. Mayer, A. F. Kreft, B. Harrison, M. Abou-gharbia, M. Antane, S. Aschmies, K. Atchison, M. Chlenov, D. C. Cole, T. Comery, G. Diamantidis, J. Ellingboe, K. Fan, R. Galante, C. Gonzales, D. M. Ho, M. E. Hoke, Y. Hu, D. Huryn, U. Jain, M. Jin, K. Kremer, D. Kubrak, M. Lin, P. Lu, R. Magolda, R. Martone, W. Moore, A. Oganesian, M. N. Pangalos, A. Porte, P. Reinhart, L. Resnick, D. R. Riddell, J. Sonnenberg-Reines, J. R. Stock, S-C Sun, E. Wagner, T. Wang, K. Woller, Z. Xu, M. M. Zaleska, J. Zeldis, M. Zhang, H. Zhou and J. S. Jacobsen, J.Med.Chem, 51 (23), pp 7348-73-51 (2008).
  7. "Enhanced Clearance of Aβ in Bran by Sustaining the Plasmin Proteolysis Cascade," J. S. Jacobsen, T.A. Comery, R. L. Martone, H. Elokdah, D. L. Crandall, A. Organesian, S.Aschmies, Y. Kirksey, C. Gonzales, J. Zu, H. Zhou, K. Atchison, E. Wagner, M. M. Zaleska, I. Das, R.L. Arias, J. Bard, D. Riddell, S. J. Gardell, M.A. Abou-Gharbia, A. Robichaud, R. Magolda, G. P. Vlasuk, T. Bjornsson, P. H. Reinhart, and M. N. Pangalos, PNAS, 105:8754-8759 (2008).
  8. "Binding of Rapamycin Analogs to Calcium Channels and FKBP52 contributes to their neuroprotective activities," B. Ruan, K. Pong, F. Jow, M. Bowlby, R.A. Crozier, D. Liu, S. Liang, Y. Chen, M.L. Mercado, X. Feng, F. Bennett, D. von Schack, L. McDonald, M. M. Zaleska, A. Wood, P.H. Reinhart, R. L. Magolda, J. Skotnicki, M.N. Pangalos, F. E. Koehn, G. T. Carter, M. Abou-Gharbia, E. I. Graziani, Proc. Natl. Acad. Sci.105:33-38 (2008).
  9. "Lecozotan Hydrochloride: Cognition Enhancer, Treatment for Alzheimer's Disease-Competitive 5-HT1A Receptor Antagonist," W.E. Childers, Jr., B.L. Harrison, M.A. Abou-Gharbia, S. Raje, V. Parks, M.N. Pangalos, and L.E. Schechter, Drugs of the Future, 32 (2007).
  10. "Desvenlafaxine Succinate: A New Seratonin And Noreprinephrine Reuptake Inhibitor", D. C. Deechey, C. E. Beyer, G. Johnston, J. Bray. S. Sah, M. Abou-Gharbia, J. Pharmacol. Exp. Ther., 318 (2), 657-65 (2006).
  11. "Lecozotan (SRA-333): A Selective Serotonin 1A Receptor Antagonist That enhances the Stimulated Release of Glutamate and Acetylcholine in the Hippocampus and Possesses Cognitive-Enhancing Properties," L.E. Schechter, D.L. Smith, S. Rosenzweig-Lipson, S.J. Sukoff, L.A. Dawson, K. Marquis, D. Jones, M. Piesla, T. Andree, S. Nawoschik, J.A. Harder, M.D. Womack, J. Buccafusco, A.V. Terry, B. Hoebel, P. Rada, M. Kelly, M. Abou-Gharbia, J.E. Barrett, and W. Childers, JPET 314:1274-1289 (2005).
  12. "Synthesis and Biological Evaluation of Benzodioxanyl-Piperazine Derivatives as Potent Serotonin 5-HT1A Antagonists: The Discovery of Lecozotan," W.E. Childers, Jr., M.G. Kelly, M.A. Abou-Gharbia, T.H. Andree, B.L. Harrison, G. Hornby, L. Potestio, S.J. Rosenzweig-Lipson, J. Schmid, D.L. Smith, S.J. Sukoff, G. Zhang and L.E. Schecter, J. Med. Chem., 48:10, 3467-3470 (2005).
  13. "Tiplaxtinin, a Novel, Orally Efficacious PAI-1 Inhibitor: Design, Synthesis, and Preclinical Characterization", H. Elokdah, M. Abou-Gharbia, J. K. Hennan, G. McFarlane, C. P. Mugford, G. Krishnamurthy, and D. L. Crandall, J. Med. Chem., 47, 3491-3494 (2004).
  14. "Design, Synthesis, and Biological Evaluation of Thio-Containing Compounds with Serum HDL-Cholesterol-Elevating Properties," H. Elokdah, T.S. Sulkowski, M. Abou-Gharbia, J.A. Butera, S.Y. Chai, G.R. McFarlane, M-L. McKean, J.L. Babiak, S.J. Adelman and E.M. Quinet, J. Med. Chem., 47, 681-695 (2004).
  15. "Optimization of Natural Product Leads into Drug Candidates", M. Abou-Gharbia, Chapter in Biodiversity, Kluwer Academic/Plenum Pub., 60-70 (2002).
  16. "EAA-090", W.E. Childers, M.A. Abou-Gharbia, J.A. Moyer, M.M. Zaleska, Drugs of the Future, 27 (7), 633-638 (2002).


Dr. Daniel Canney

  1. Desai, S., Sun, W., Gabriel, J. L., and Canney, D. J., The Synthesis and Preliminary Evaluation of Substituted Chromones, Coumarins, Chromanones, and Benzophenomones as Retinoic Acid Receptor Ligands. Heterocyclic Communications, 2008, 14:3 129-137.
  2. Sun, W., Desai, S., Piao, H., Carroll, P., Canney, D.J., Wittig-Horner-Emmons Reactions of Triethyl-3-methyl-phosphonocrotonate with 3-Formylchromones en Route to Benzophenone-Based Retinoid Candidates, Heterocycles, 2007, 71:3, 557-567.
  3. Tao, X., Piao, H., Canney, D. J., Borenstein, M.R., Nnane, I.P. "Biotransformation of Letrazole in Rat Microsomes: Effects of Gender and Tamoxifen" , J. Pharmaceutical and Biomed Analysis, 2006, 43, 1078-1085.
  4. Ahungena, A., Canney, D. J. Synthesis and Evaluation of Homologous Analogs of Anticonvulsant 5-Substituted 3,3-Diethyl-4,5-Dihydro-2(3)-Furanones. Medicinal Chemistry Research, 2005, 14:7, 404-428.
  5. Sun, W., Blanton, M. P., Gabriel, J. L., Canney, D. J. .Bioisosteric Replacement in the Design and Synthesis of Ligands for Nicotinic Acetylcholine Receptors. Medicinal Chemistry Research, 2005, 14:5, 241-259.
  6. Ahungena, A., Gabriel, J. L., Canney, D. J. Synthesis and Evaluation of 5-Substituted Derivatives of 4,5 Dihydro-3,3,-Diethyl-2-(3H)-Furanone as Subtype-Selective Muscarinic Leads. Medicinal Chemistry Research, 2003, 12:9, 481-511.
  7. Canney, D. J., Buccafusco, J., Zhang, M., Doukas, P. H., Characterization of Ethyl (3-quinuclidinyl) acetate (EQA) as a Ligand for Cholinergic Receptors. Life Sciences, Pharmacology Letters, 1998, 63:24, PL 329-336.
  8. Canney, D. J., Lu, H-F., Holland, K. D., McKeon, A. C., Ferrendelli, J. A., and Covey, D.F. Synthesis and Evaluation of Fluorinated γ-Butyrolactones and γ-Thiobutyrolactones as Modulators of the GABA Receptor Complex. Bioorg. Med. Chem., 1998, 6, 43-55.


Dr. Marc Ilies

  1. M.A. Ilies, W.A. Seitz, B.H. Johnson, E.L. Ezell, A.L. Miller, E.B. Thompson, A.T. Balaban, "Lipophilic Pyrylium Salts in the Synthesis of Efficient Pyridinium-Based Cationic Lipids, Gemini Surfactants, and Lipophilic Oligomers for Gene Delivery", J. Med. Chem., 49, 3872-3887 (2006).
  2. V. Percec, M. Peterca, M.J. Sienkowska, M.A. Ilies, E. Aqad, J. Smidrkal, P.A. Heiney, "Synthesis and Retrostructural Analysis of Libraries of AB3 and Constitutional Isomeric AB2 Phenylpropyl Ether-Based Supramolecular Dendrimers", J. Am. Chem. Soc., 128, 3324-3334 (2006).
  3. M.A. Ilies, B.H. Johnson, F. Makori, A. Miller, W.A. Seitz, E.B. Thompson, A.T. Balaban, "Pyridinium cationic lipids in gene delivery: An in vitro and in vivo comparison of transfection efficiency versus a tetraalkylammonium congener", Arch. Biochem. Biophys., 435, 217-226 (2005).
  4. M.A. Ilies, W.A. Seitz, I. Ghiviriga, B.H. Johnson, A. Miller, E.B. Thompson, A.T. Balaban, "Pyridinium cationic lipids in gene delivery: a structure-activity correlation study", J. Med. Chem., 47, 3744-3754 (2004).
  5. M.A. Ilies, B. Masereel, S. Rolin, A. Scozzafava, G. Câmpeanu, V. Cîmpeanu, C.T. Supuran, "Carbonic anhydrase inhibitors: Aromatic and heterocyclic sulfonamides incorporating adamantyl moieties with strong anticonvulsant activity", Bioorg. Med. Chem., 12, 2717-2726 (2004).
  6. M.A. Ilies, W.A. Seitz, M.T. Caproiu, M. Wentz, R.E. Garfield and A.T. Balaban, "Pyridinium-Based Cationic Lipids as Gene Transfer Agents", Eur. J. Org. Chem., 14, 2645-2655 (2003).
  7. [M.A. Ilies] "Novel tripeptide inhibitors of hepatitis C virus NS3 serine protease. Bristol-Myers Squibb Co.: WO02060926", Expert Opin. Ther. Patents, 13 (2), 267-272 (2003) - patent evaluation.
  8. M.A. Ilies, D. Vullo, J. Pastorek, A. Scozzafava, M. Ilies, M.T. Caproiu, S. Pastorekova and C.T. Supuran, "Carbonic anhydrase inhibitors. Inhibition of tumor-associated isozyme IX by halogenosulfanilamide and halogeno-aminobenzolamide derivatives", J. Med. Chem., 46, 2187-2196 (2003).