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PUBLICATIONS

  1. Meegalla, S. K., Wall, M. J., Chen, J., Wilson, K. J., Ballentine, S. K., DesJarlais, R. L., Schubert, C., Crysler, C. S., Chen, Y., Molloy, C. J., Chaikin, M. A., Manthey, C. L., Player, M. R., Tomczuk, B. E., Illig, C. R., “Structure-based optimization of a potent class of arylamide FMS inhibitors”, Bioorganic & Medicinal Chemistry Letters, 2008, 18, 3632-363.

  2. Kreutter, K. D., Lu, T., Lee, L., Giardino, E. C., Patel, S., Huang, H., Xu, Fitzgerald, G. M., Haertlein, B. J., Mohan, V., Crysler, C., Eisennagel, S., Dasgupta, M., McMillan, M., Spurlino, J. C., Huebert, N. D., Maryanoff, B. E., Tomczuk, B. E., Damiano, B. P., Player, M. R., “Orally efficacious thrombin inhibitors with cyanofluorophenylacetamide as the P2 motif”, Bioorganic & Medicinal Chemistry Letters, 2008, 18, 2865-2870.

  3. Wall, M. J., Chen, J., Meegalla, S., Ballentine, S. K., Wilson, K. J.,  DesJarlais, R. L., Schubert, C., Chaikin, M. A., Crysler, C., Petrounia, I. P., Donatelli, R. R., Yurkow, E. J., Boczon, L., Mazzulla, M., Player, M. R., Patch, R. J., Manthey, C. L., Molloy, C., Tomczuk, B., Illig, C. R., “Synthesis and evaluation of novel 3,4,6-substituted 2-quinolones as FMS kinase inhibitors”, Bioorganic & Medicinal Chemistry Letters, 2008, 18,2097-2102.

  4. Winters, M. P., Crysler, C., Subasinghe, N., Ryan, D., Leong, L., Zhao, S., Donatelli, R., Yurkow, E., Mazzulla, M., Boczon, L., Manthey, C., Molloy, C., Raymond, H., Murray, L., McAlonan, L., Tomczuk, B., “Carboxylic Acid Bioisosteres Acylsulfonamides, Acylsulfamides, and Sulfonylureas, as Novel Antagonists of the CXCR2 Receptor”, Bioorganic & Medicinal Chemistry Letters, 2008, 18, 1926-1930.

  5. Chen, Y., Cheng, D., Marugan, J.J., Manthey, C., Tomczuk, B., Huebert, N., “Pharmacokinetics of TDP223206 following intravenous and oral administration to intact rats and intravenous administration to bile duct-cannulated rats”, Biopharmaceutics and Drug Disposition, 2008, 29, 219-230.

  6. Illig, C. R., Chen, J., Wall, M. J., Wilson, K. J., Ballentine, S. K., Rudolph, M. J., DesJarlais, R. L., Chen, Y., Schubert, C., Petrounia, I., Crysler, C. S., Molloy, C. J., Chaikin, M. A., Manthey, C. L., Player, M. R., Tomczuk, B. E., Meegalla, S. K., “Discovery of novel FMS kinase inhibitors as anti-inflammatory agents”, Bioorganic & Medicinal Chemistry Letters, 2008, 18,1642-1648.

  7. Travins, J. M., Ali, F., Huang, H., Ballentine, S. K., Khalil, E., Hufnagel, H. R/. Pan, W., Gushue, J., Leonard, K., Bone, R. F., Soll, R. M., DesJarlais, R. L., Crysler, C. S., Ninan, N., Kirkpatrick, J., Cummings, M. D., Huebert, N., Molloy, C. J., Gaul, M., Tomczuk, B. E., et al., “Biphenylsulfonyl-thiophene-carboxamidine inhibitors of the complement component C1s”, Bioorganic & Medicinal Chemistry Letters, 2008, 18, 1603-1606.

  8. Illig, C. R., Chen, J., Wall, M. J., Wilson, K. J., Ballentine, S. K., Rudolph, M. J., DesJarlais, R. L., Chen, Y., Schubert, C., Petrounia, I., Crysler, C. S., Molloy, C. J., Chaikin, M. A., Manthey, C. L., Player, M. R., Tomczuk, B. E., Meegalla, S. K., “Discovery of novel FMS kinase inhibitors as anti-inflammatory agents”, Bioorganic & Medicinal Chemistry Letters, 2008, 18, 1642-1648 (2008).

  9. Chen, Y., Cheng, D., Tio, C., Kagan, N., Eisennagel, S., Dasgupta, M., Tomczuk, B., Bone, R., Huebert, N., “Pharmacokinetic Properties of TDP4815 after Single Intravenous and Oral Administrations to Rat, Rabbit, Monkey, Dog and in Vitro Drug Metabolism”, Biopharmaceutics and Drug Disposition, 2008, 29 (3), 127-138.

  10. Lee, L., Kreutter, K. D., Pan, W., Crysler, C., Spurlino, J., Player, M., Tomczuk, B., Lu, T., “2-(2-Chloro-6-Fluorophenyl)Acetamides as Potent Thrombin Inhibitors”, Bioorganic & Medicinal Chemistry Letters, 2007, 17, 6266-6299.

  11. Raboisson, P., DesJarlais, R., Reed, R., Lattanze, J., Chaikin, M., Manthey, C., Tomczuk, B., Marugan, J.J., “Identification of novel short chain 4-substituted indoles as potent alpha(v)beta(3) antagonists using structure-based drug design”, European Journal of Medicinal Chemistry, 2007, 42, 334-343.

  12. Raboisson, Pierre; Manthey, Carl L.; Chaikin, Margery; Lattanze, Jennifer; Crysler, Carl; Leonard, Kristi; Pan, Wenxi; Tomczuk, Bruce E.; Marugan, Juan Jose, “Novel potent and selective a vb 3/a vb 5 integrin dual antagonists with reduced binding affinity for human serum albumin”, European Journal of Medicinal Chemistry, 2006, 41, 847-861.

  13. Subasinghe, Nalin L.; Travins, Jeremy M.; Ali, Farah; Huang, Hui; Ballentine, Shelley K.; Marugan, Juan Jose; Khalil, Ehab; Hufnagel, Heather R.; Bone, Roger F.; DesJarlais, Renee L.; Crysler, Carl S.; Ninan, Nisha; Cummings, Maxwell D.; Molloy, Christopher J.; Tomczuk, Bruce E., “A novel series of arylsulfonylthiophene-2-carboxamidine inhibitors of the complement component C1s”, Bioorganic & Medicinal Chemistry Letters, 2006, 16, 2200-2204.

  14. Chaikin, M. A., Marugan, J. J., DeVries, G. W., Baciu, P., Edelman, J., Ni, M., Tomczuk, B. E., Pan, W., Guo, Z., Anaclerio, B., Leonard, K., Eisennagel, S. H., Molloy, C. J., Manthey, C. L., “A functional radioreceptor assay of alpha-V-beta-3 (avb3) inhibitors in plasma: Application as an ex vivo pharmacodynamic model”, Journal of Biochemical and Biophysical Methods, 2005, 65, 107-120.

  15. Qiao, L., Baumann, C., Crysler, C., Ninan, N., Abad, M., Spurlino, J., DesJarlais, R., Kervinen, J., Neeper, M., Bayoumy, S., Williams, R., Deckman, I., Dasgupta, M., Reed, R., Huebert, N., Tomczuk, B., Moriarty, K., “Discovery, SAR, and X-ray structure of novel biaryl-based dipeptidyl peptidase IV inhibitors”, Bioorg. Med. Chem. Lett., 2006, 16, 123-128.

  16. Leonard, K., Pan, W., Anaclerio, B., Gushue, J., Guo, Z., DesJarlais, R., Chaikin, M., Lattanze, J., Crysler, C., Manthey, C., Tomczuk, B., Marugan, J.J., “Non-peptidic avb3 antagonists containing indol-1-yl propionic acids”, Bioorg. Med. Chem. Lett., 2005, 15, 2679-2684.

  17. Grasberger, B., Lu, T., Schubert, C., Parks, D., Carver, T., Koblish, H., Cummings, M. D., LaFrance, L., Milkiewicz, K. L., Calvo, R. R., Maguire, D., Lattanze, J., Franks, C/ F., Zhao, S., Ramachandren, K., Bylebyl, G. R., Zhang, M., Manthey, C. L., Petrella, E. C., Pantaliano, M. W., Deckman, I. C., Spurlino, J. C., Maroney, A. C., Tomczuk, B. E., Molloy, C. J., Bone, R. F. “Discovery and Cocrystal Structure of Benzodiazepinone HDM2 Antagonists That Activate p53 in Cells”, J. Med. Chem., 2005, 48, 909-912.

  18. Marugan, J. J., Manthey, C., Anaclerio, B., LaFrance, L., Crysler, C., Ninan, N., Abad, M., Spurlino, J., DesJarlais, R., Kervinen, J., Neeper, M., Bayoumy, S., Williams, R., Deckman, I., Tomczuk, B., Moriarty, K. “Design, Synthesis, and Biological Evaluation of Novel Potent and Selective avb3/avb5 Integrin Dual Inhibitors with Improved Bioavailability. Selection of the Molecular Core” J. Med. Chem., 2005, 48, 926-934.

  19. Lu, T., Markotan, T., Coppo, F., Tomczuk, B., Crysler, C., Eisennagel, S., Spurlino, J., Gremminger, L., Soll, R., Giardino, E., Bone, R. “Oxyguanidines: Part 2. Discovery of a Novel Orally Active Thrombin Inhibitor through Structure-Based Drug Design and Parallel Synthesis”, Bioorg. Med. Chem. Lett., 2004, 14, 3727-3731.

  20. Tomczuk, B., Lu, T., Soll, R.M., Fedde, C., Wang, A., Murphy, L., Crysler, C., Dasgupta, M., Eisennagel, S., Spurlino, J., Bone, R., “Oxyguanidines:Application to Non-peptidic Phenyl-Based Thrombin Inhibitors”, Bioorg. Med. Chem. Lett., 2003, 13, 1495-1498.

  21. Lu,T., Tomczuk, B., Bone, R., Murphy, L., Salemme, F.R., Soll, R.M., "Non-Peptidic Phenyl-Based Thrombin Inhibitors: Exploring Structural Requirements of the S1 Specificity Pocket with Amidines", Bioorg. Med. Chem. Lett., 2000, 10, 83-85.

  22. Lu,T., Soll, R.M., Illig, C.R., Bone, R., Murphy, L., Spurlino, J., Salemme, F.R., Tomczuk, B., "Structure-Activity and Crystallographic Analysis of a New Class of Non-amide-Based Thrombin Inhibitor", Bioorg. Med. Chem. Lett., 2000, 10, 79-82.

  23. Soll, R.M., Lu,T., Tomczuk, B., Illig, C.R., Fedde, C., Eisennagel, S., Bone, R., Murphy, L., Spurlino, J., Salemme, F.R., "Amidinohydrazones as Guanidine Bioisosteres: Application to a  New Class of Potent, Selective and Orally Bioavailable, Non-amide-Based Small-Molecule  Thrombin Inhibitors", Bioorg. Med. Chem. Lett., 2000, 10, 1-4.

  24. Lu,T., Tomczuk, B., Illig, C.R., Bone, R., Murphy, L., Spurlino, J., Salemme, F.R., Soll, R.M., “In vitro Evaluation and Crystallographic Analysis of a new Class of Selective, Non-amide-based Thrombin Inhibitors”, Bioorg. Med. Chem. Lett., 1998, 8, 1595-1600.

  25. Enhancing the Drug Discovery Process by Integration of High-Throughput Chemistry and  Structure-Based Drug Design. Molecular Diversity and Combinatorial Chemistry, I. M. Chaiken, K. D. Janda, Eds., ACS, Washington D. C., 1996, 16-27. Todd L. Graybill, Dimitris K. Agrafiotis, Roger Bone, Carl R. Illig, Edward P. Jaeger, K. T. Locke, Tianbao Lu, J. M. Salvino, Richard M. Soll, John C. Spurlino, Nalin Subasinghe, Bruce E. Tomczuk, and F. Raymond Salemme. 

  26. Gowravaram, M. R., Johnson, J. S., Delecki, D., Cook, E. R., Tomczuk, B. E., Ghose, A. K., Mathiowetz, A. M., Spurlino, J. C., Rubin, B., Smith, D. L., Pulvino, T., Wahl, R. C., "Design and Synthesis of Novel Hydroxamate Inhibitors of the Matrix Metallo-proteinases", J. Med. Chem., 1995, 38, 2570-2581.

  27. Ghose, A. K., Logan, M. E., Treasurywala, A. M., Wang, H., Wahl, R. C., Tomczuk, B., Gowravaram, M., Jaeger, E. P., Wendoloski, J. J., "Determination of Pharmacophoric Geometry for Collagenase Inhibitors Using a Novel Computational Method and It's Verification Using Molecular Dynamics, NMR, and X-ray Crystallography", J. Am. Chem. Soc., 1995, 117, 4671-4682.

  28. Wahl, R. C., Pulvino, T., Mathiowetz, A. M., Ghose, A. K., Johnson, J. S., Delecki, D., Cook, E. R., Gainor, J. A., Gowravaram, M. R., Tomczuk, B. E., " Hydroxamate Inhibitors of Human Gelatinase B (92kDa)", Bioorg. MedChem. Lett., 1995, 5, 349-352.

  29. Tomczuk, B. E., Gowravaram, M. R., Johnson, J. S., Delecki, D., Cook, E. R., Ghose, A. K., Mathiowetz, A. M., Spurlino, J. C., Rubin, B., Smith, D. L., Pulvino, T., Wahl, R. C., "Hydroxamate Inhibitors of the Matrix Metallo-proteinases (MMPs) Containing Heteroatom Based Modifications of the P1' Group", Bioorg. MedChem. Lett., 1995, 5, 343-348.

  30. Lawrence, K. B., Venepalli, B. R., Appell, K. C., Goswami, R., Logan, M. E., Tomczuk, B. E., Yanni, Y. M., "Synthesis and Substance P Antagonist Activity of Naphthimidazolium Derivatives", J. Med. Chem., 1992,35, 1273-1279.

  31. Venepalli, B. R., Aimone, L. D., Appell, K. C., Bell, M. R., Dority, J. A., Goswami, R., Hall, P. L., Kumar, V., Lawrence, K. B., Logan, M. E., Scensny, P. M., Seelye, J. A., Tomczuk, B. E., Yanni, J. M., "Synthesis and Substance P Receptor Binding Activity of Androstano[3,2-b](pyrimido[1,2-a]benzimidazoles)", J. Med. Chem., 1992, 35, 374-378.

  32. Appell, K. C., Fragale, B. J., Loscig, J., Singh, S., Tomczuk, B. E., "Antagonists that Demonstrate Species Differences of Neurokinin-1 Receptors", Mol. Pharmacol., 1992, 41, 772-778.

  33. Appell, K. C., Babb, B., Goswami, R., Hall, P. L., Lawrence, K. B., Logan, M. E., Przyklek-Elling, R., Tomczuk, B. E., Venepalli, B. R., Yanni, Y. M., "Imidazo[4,5-b]quinoxaline cyanines as neurokinin antagonists", J. Med. Chem., 1991, 34, 1751-1753.

  34. Logan, M. E., Goswami, R., Tomczuk, B. E., and Venepalli, B. R., "Recent Advances in Neurokinin Receptor Antagonists", Ann. Rep. Med. Chem. 1991, 26, 43-51.

  35. Tomczuk, B. E., Taylor, C. R.,Jr., Moses, L. M., Sutherland, D. B., Johnson, D. N., Kinnier, W. B., and Kilpatrick, B. F., "2-Phenyl-3H-imidazo[4,5-b]pyridine-3-acetamides as non-benzodiazepine anticonvulsants and anxiolytics", J. Med. Chem., 1991, 34, 2993-3006.

  36. Tomczuk, B. E., Logan, M. E., Venepalli, B. R., and Goswami, R., "Neurokinin receptor ligands", Current Opinion in Therapeutic Patents, 1991, 1, 197-210.

  37. Wagner, L. E., Tomczuk, B. E., and Yanni, J. M., "Measurement of Tachykinin-Induced Salivation in Conscious Rats", J. Pharmacol. Methods, 1991, 26, 67-72.


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