B. Tomczuk

发表

Determination of Pharmacophoric Geometry for Collagenase Inhibitors Using a Novel Computational Method and Its Verification Using Molecular Dynamics, NMR, and X-ray Crystallography

A. Ghose, M. Logan, A. Treasurywala, 1995 .

Discovery and cocrystal structure of benzodiazepinedione HDM2 antagonists that activate p53 in cells.

Maxwell D Cummings, B. Tomczuk, J. Spurlino, 2005, Journal of medicinal chemistry.

Current ADC Linker Chemistry

B. Tomczuk, Nareshkumar Jain, S. Smith, 2015, Pharmaceutical Research.

Enhancement of kinase selectivity in a potent class of arylamide FMS inhibitors.

B. Tomczuk, R. DesJarlais, S. Meegalla, 2013, Bioorganic & medicinal chemistry letters.

Unmet Medical Needs

B. Tomczuk, 2014, Inflammation Research.

Pharmacokinetic properties of TDP4815 after single intravenous and oral administrations to rat, rabbit, monkey, dog and in vitro drug metabolism

B. Tomczuk, R. Bone, Yanmin Chen, 2008, Biopharmaceutics & drug disposition.

Non-peptidic αvβ3 antagonists containing indol-1-yl propionic acids

B. Tomczuk, R. DesJarlais, J. Marugan, 2005 .

Effect of the Mammalian Arginase Inhibitor 2(S)-Amino-6-Boronohexanoic Acid on Bacillus anthracis Arginase

B. Tomczuk, P. Suzdak, P. Shapiro, 2012, Current Microbiology.

Antagonists that demonstrate species differences in neurokinin-1 receptors.

B. Tomczuk, K. Appell, B. J. Fragale, 1992, Molecular pharmacology.

Reducing ion channel activity in a series of 4-heterocyclic arylamide FMS inhibitors.

B. Tomczuk, R. DesJarlais, S. Meegalla, 2010, Bioorganic & medicinal chemistry letters.

Carboxylic acid bioisosteres acylsulfonamides, acylsulfamides, and sulfonylureas as novel antagonists of the CXCR2 receptor.

B. Tomczuk, D. Ryan, Shuyuan Zhao, 2008, Bioorganic & medicinal chemistry letters.

Hydroxamate inhibitors of human gelatinase B (92 kDa)

A. Ghose, R. Wahl, B. Tomczuk, 1995 .

Discovery, SAR and X-ray structure of 1H-benzimidazole-5-carboxylic acid cyclohexyl-methyl-amides as inhibitors of inducible T-cell kinase (Itk).

B. Tomczuk, R. DesJarlais, D. Ryan, 2008, Bioorganic & medicinal chemistry letters.

Hydroxamate inhibitors of the matrix metallo-proteinases (MMPs) containing novel P1′ heteroatom based modifications

A. Ghose, R. Wahl, B. Tomczuk, 1995 .

A functional radioreceptor assay of alpha-V-beta-3 (αvβ3) inhibitors in plasma: Application as an ex vivo pharmacodynamic model

B. Tomczuk, J. Marugan, C. Manthey, 2005 .

Chapter 5. Recent Advances in Neurokinin Receptor Antagonists

M. Logan, B. Tomczuk, R. Goswami, 1991 .

JNJ-28312141, a novel orally active colony-stimulating factor-1 receptor/FMS-related receptor tyrosine kinase-3 receptor tyrosine kinase inhibitor with potential utility in solid tumors, bone metastases, and acute myeloid leukemia

B. Tomczuk, S. Meegalla, C. Illig, 2009, Molecular Cancer Therapeutics.

Non-peptidic phenyl-based thrombin inhibitors: exploring structural requirements of the S1 specificity pocket with amidines.

B. Tomczuk, F. Salemme, R. Bone, 2000, Bioorganic & medicinal chemistry letters.

Amidinohydrazones as guanidine bioisosteres: application to a new class of potent, selective and orally bioavailable, non-amide-based small-molecule thrombin inhibitors.

B. Tomczuk, J. Spurlino, C. Illig, 2000, Bioorganic & medicinal chemistry letters.

In vitro evaluation and crystallographic analysis of a new class of selective, non-amide-based thrombin inhibitors.

B. Tomczuk, J. Spurlino, C. Illig, 1998, Bioorganic & medicinal chemistry letters.

Oxyguanidines. Part 2: Discovery of a novel orally active thrombin inhibitor through structure-based drug design and parallel synthesis.

B. Tomczuk, J. Spurlino, Tianbao Lu, 2004, Bioorganic & medicinal chemistry letters.

Oxyguanidines: application to non-peptidic phenyl-based thrombin inhibitors.

B. Tomczuk, J. Spurlino, Tianbao Lu, 2003, Bioorganic & medicinal chemistry letters.

Structure-activity and crystallographic analysis of a new class of non-amide-based thrombin inhibitor.

B. Tomczuk, J. Spurlino, C. Illig, 2000, Bioorganic & medicinal chemistry letters.

In vitro Evaluation and Crystallographic Analysis of a New Class of Selective, Non‐Amide‐Based Thrombin Inhibitors.

B. Tomczuk, J. Spurlino, C. Illig, 1998 .

Amidinohydrazones as Guanidine Bioisosteres: Application to a New Class of Potent, Selective and Orally Bioavailable, Non‐amide‐based Small‐Molecule Thrombin Inhibitors.

B. Tomczuk, J. Spurlino, C. Illig, 2000 .

Orally efficacious thrombin inhibitors with cyanofluorophenylacetamide as the P2 motif.

B. Tomczuk, J. Spurlino, Hui-Sheng Huang, 2008, Bioorganic & medicinal chemistry letters.

Discovery and clinical evaluation of 1-{N-[2-(amidinoaminooxy)ethyl]amino}carbonylmethyl-6-methyl-3-[2,2-difluoro-2-phenylethylamino]pyrazinone (RWJ-671818), a thrombin inhibitor with an oxyguanidine P1 motif.

B. Tomczuk, J. Spurlino, Tianbao Lu, 2010, Journal of medicinal chemistry.

Synthesis and substance P antagonist activity of naphthimidazolium derivatives.

M. Logan, B. Tomczuk, J. Yanni, 1992, Journal of medicinal chemistry.

Imidazo[4,5-b]quinoxaline cyanines as neurokinin antagonists.

M. Logan, B. Tomczuk, J. Yanni, 1991, Journal of medicinal chemistry.

Design, Synthesis, and Biological Evaluation of Novel Potent and Selective αvβ3/αvβ5 Integrin Dual Inhibitors with Improved Bioavailability. Selection of the Molecular Core

B. Tomczuk, Tianbao Lu, J. Marugan, 2005 .

2-Phenyl-3H-imidazo[4,5-b]pyridine-3-acetamides as non-benzodiazepine anticonvulsants and anxiolytics.

B. Tomczuk, Y. Lo, C. Taylor, 1991, Journal of medicinal chemistry.

Synthesis and evaluation of novel 3,4,6-substituted 2-quinolones as FMS kinase inhibitors.

B. Tomczuk, R. DesJarlais, S. Meegalla, 2008, Bioorganic & medicinal chemistry letters.

Discovery of novel FMS kinase inhibitors as anti-inflammatory agents.

B. Tomczuk, R. DesJarlais, S. Meegalla, 2008, Bioorganic & medicinal chemistry letters.

2-(2-Chloro-6-fluorophenyl)acetamides as potent thrombin inhibitors.

Mark R Player, B. Tomczuk, J. Spurlino, 2007, Bioorganic & medicinal chemistry letters.

Original articleNovel potent and selective αvβ3/αvβ5 integrin dual antagonists with reduced binding affinity for human serum albumin

Juan J. Marugan, B. Tomczuk, J. Marugan, 2006 .

Effect of the Mammalian Arginase Inhibitor 2(S)-Amino-6-Boronohexanoic Acid on Bacillus anthracis Arginase

B. Tomczuk, P. Suzdak, P. Shapiro, 2012, Current Microbiology.

1H‐Pyrazole‐1‐carboxamidine Hydrochloride

B. Tomczuk, M. Bernatowicz, 2008 .

Discovery, SAR, and X-ray structure of novel biaryl-based dipeptidyl peptidase IV inhibitors.

B. Tomczuk, R. DesJarlais, J. Spurlino, 2006, Bioorganic & medicinal chemistry letters.

Measurement of tachykinin-induced salivation in conscious rats.

B. Tomczuk, J. Yanni, L. Wagner, 1991, Journal of pharmacological methods.

Current ADC Linker Chemistry

B. Tomczuk, Nareshkumar Jain, S. Smith, 2015, Pharmaceutical Research.

Identification of novel short chain 4-substituted indoles as potent αvβ3 antagonist using structure-based drug design

B. Tomczuk, R. DesJarlais, J. Marugan, 2007 .

Pharmacokinetics of TDP223206 following intravenous and oral administration to intact rats and intravenous administration to bile duct‐cannulated rats

B. Tomczuk, J. Marugan, C. Manthey, 2008, Biopharmaceutics & drug disposition.

Optimization of a potent class of arylamide colony-stimulating factor-1 receptor inhibitors leading to anti-inflammatory clinical candidate 4-cyano-N-[2-(1-cyclohexen-1-yl)-4-[1-[(dimethylamino)acetyl]-4-piperidinyl]phenyl]-1H-imidazole-2-carboxamide (JNJ-28312141).

B. Tomczuk, R. DesJarlais, S. Meegalla, 2011, Journal of medicinal chemistry.

Structure-based optimization of a potent class of arylamide FMS inhibitors.

Jinsheng Chen, Mark R Player, B. Tomczuk, 2008, Bioorganic & medicinal chemistry letters.

Inhibition of matrix metalloproteinases by hydroxamates containing heteroatom-based modifications of the P1' group.

J. S. Johnson, A. Ghose, B. Tomczuk, 1995, Journal of medicinal chemistry.

Design and synthesis of polyethylene glycol-modified biphenylsulfonyl-thiophene-carboxamidine inhibitors of the complement component C1s.

B. Tomczuk, C. Molloy, R. Bone, 2012, Bioorganic & medicinal chemistry letters.

Biphenylsulfonyl-thiophene-carboxamidine inhibitors of the complement component C1s.

B. Tomczuk, R. DesJarlais, Hui-Sheng Huang, 2008, Bioorganic & medicinal chemistry letters.

A novel series of arylsulfonylthiophene-2-carboxamidine inhibitors of the complement component C1s.

B. Tomczuk, R. DesJarlais, Hui-Sheng Huang, 2006, Bioorganic & medicinal chemistry letters.

Discovery of novel FMS kinase inhibitors as anti-inflammatory agents.

B. Tomczuk, R. DesJarlais, S. Meegalla, 2008, Bioorganic & medicinal chemistry letters.