J. Bouska

发表

Thienopyrimidine ureas as novel and potent multitargeted receptor tyrosine kinase inhibitors.

K. Glaser, S. Davidsen, V. Stoll, 2005, Journal of medicinal chemistry.

Discovery of N-(4-(3-amino-1H-indazol-4-yl)phenyl)-N'-(2-fluoro-5-methylphenyl)urea (ABT-869), a 3-aminoindazole-based orally active multitargeted receptor tyrosine kinase inhibitor.

K. Glaser, S. Davidsen, V. Stoll, 2007, Journal of medicinal chemistry.

Design, synthesis, and biological activity of 5,10-dihydro-dibenzo[b,e][1,4]diazepin-11-one-based potent and selective Chk-1 inhibitors.

Chang Park, John Xue, Saul H Rosenberg, 2007, Journal of medicinal chemistry.

Preclinical Characterization of ABT-348, a Kinase Inhibitor Targeting the Aurora, Vascular Endothelial Growth Factor Receptor/Platelet-Derived Growth Factor Receptor, and Src Kinase Families

K. Glaser, S. Davidsen, C. Tse, 2012, Journal of Pharmacology and Experimental Therapeutics.

Synthesis and SAR of novel tricyclic quinoxalinone inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1).

Eric F. Johnson, X. Liu, V. Giranda, 2009, Bioorganic & medicinal chemistry letters.

The PARP inhibitor, ABT-888 potentiates temozolomide: correlation with drug levels and reduction in PARP activity in vivo.

Eric F. Johnson, X. Liu, V. Giranda, 2008, Anticancer research.

Discovery of trans-3,4'-bispyridinylethylenes as potent and novel inhibitors of protein kinase B (PKB/Akt) for the treatment of cancer: Synthesis and biological evaluation.

V. Stoll, Eric F. Johnson, X. Liu, 2006, Bioorganic & medicinal chemistry letters.

Cyanopyridyl containing 1,4-dihydroindeno[1,2-c]pyrazoles as potent checkpoint kinase 1 inhibitors: improving oral biovailability.

Philip J. Merta, Gaoquan Li, Z. Tao, 2007, Bioorganic & medicinal chemistry letters.

Discovery of 3H-benzo[4,5]thieno[3,2-d]pyrimidin-4-ones as potent, highly selective, and orally bioavailable inhibitors of the human protooncogene proviral insertion site in moloney murine leukemia virus (PIM) kinases.

V. Stoll, Eric F. Johnson, N. Soni, 2009, Journal of medicinal chemistry.

1,4-Dihydroindeno[1,2-c]pyrazoles with acetylenic side chains as novel and potent multitargeted receptor tyrosine kinase inhibitors with low affinity for the hERG ion channel.

S. Davidsen, G. Gintant, Eric F. Johnson, 2007, Journal of medicinal chemistry.

Identification of aminopyrazolopyridine ureas as potent VEGFR/PDGFR multitargeted kinase inhibitors.

K. Glaser, S. Davidsen, N. Soni, 2008, Bioorganic & medicinal chemistry letters.

Exploration of diverse hinge-binding scaffolds for selective Aurora kinase inhibitors.

K. Glaser, S. Davidsen, N. Soni, 2012, Bioorganic & medicinal chemistry letters.

Discovery of potent and selective thienopyrimidine inhibitors of Aurora kinases.

K. Glaser, S. Davidsen, C. Abad-Zapatero, 2011, Bioorganic & medicinal chemistry letters.

Correlation of tumor growth suppression and methionine aminopetidase-2 activity blockade using an orally active inhibitor

Qian Zhang, L. Tucker, Jieyi Wang, 2008, Proceedings of the National Academy of Sciences.

Discovery and characterization of the potent, selective and orally bioavailable MMP inhibitor ABT-770.

S. Davidsen, M. Michaelides, P. Tapang, 2001, Bioorganic & Medicinal Chemistry Letters.

Improving the in vivo duration of 5-lipoxygenase inhibitors: application of an in vitro glucuronosyltransferase assay.

C. Goodfellow, G. Carter, J. Bouska, 1997, Drug metabolism and disposition: the biological fate of chemicals.

Pyrazole diaminopyrimidines as dual inhibitors of KDR and Aurora B kinases.

K. Glaser, C. Tse, M. Michaelides, 2012, Bioorganic & medicinal chemistry letters.

Thienopyridine ureas as dual inhibitors of the VEGF and Aurora kinase families.

K. Glaser, S. Davidsen, C. Tse, 2012, Bioorganic & medicinal chemistry letters.

Thienopyridine urea inhibitors of KDR kinase.

K. Glaser, S. Davidsen, N. Soni, 2007, Bioorganic & medicinal chemistry letters.

Identification of a novel 3,5-disubstituted pyridine as a potent, selective, and orally active inhibitor of Akt1 kinase.

Eric F. Johnson, X. Liu, V. Giranda, 2006, Bioorganic & medicinal chemistry letters.

Biaryl ether retrohydroxamates as potent, long-lived, orally bioavailable MMP inhibitors.

S. Davidsen, M. Michaelides, D. Albert, 2001, Bioorganic & medicinal chemistry letters.

Purification of a mammalian 5-lipoxygenase from rat basophilic leukemia cells.

A. Goetze, G. Carter, D. Bornemeier, 1985, Prostaglandins.

Synthesis and SAR of indazole-pyridine based protein kinase B/Akt inhibitors.

Eric F. Johnson, X. Liu, V. Giranda, 2006, Bioorganic & medicinal chemistry.

Isothiazolopyrimidines and isoxazolopyrimidines as novel multi-targeted inhibitors of receptor tyrosine kinases.

K. Glaser, S. Davidsen, M. Michaelides, 2006, Bioorganic & medicinal chemistry letters.

Identification of genes that confer tumor cell resistance to the Aurora B kinase inhibitor, AZD1152

K. Glaser, O. Shah, P. Tapang, 2009, The Pharmacogenomics Journal.

Optimization of phenyl-substituted benzimidazole carboxamide poly(ADP-ribose) polymerase inhibitors: identification of (S)-2-(2-fluoro-4-(pyrrolidin-2-yl)phenyl)-1H-benzimidazole-4-carboxamide (A-966492), a highly potent and efficacious inhibitor.

Eric F. Johnson, X. Liu, V. Giranda, 2010, Journal of medicinal chemistry.

Substituted 4-amino-1H-pyrazolo[3,4-d]pyrimidines as multi-targeted inhibitors of insulin-like growth factor-1 receptor (IGF1R) and members of ErbB-family receptor kinases.

S. Davidsen, Eric F. Johnson, J. Wilsbacher, 2010, Bioorganic & medicinal chemistry letters.

Physiologically relevant metal cofactor for methionine aminopeptidase-2 is manganese.

D. Egan, Chang H. Park, J. Henkin, 2003, Biochemistry.

ABT-869 a Multi-Targeted Receptor Tyrosine Kinase Inhibitor: Inhibition of FLT3 Phosphorylation and Signaling in Acute Myeloid Leukemia Running Title: ABT-869 Receptor Tyrosine Kinase Inhibitor in AML

K. Glaser, S. Davidsen, Eric F. Johnson, 2007 .

ABT-888 , an OrallyActive Poly ( ADP-Ribose ) Polymerase Inhibitor that Potentiates DNA-Damaging Agents in PreclinicalTumorModels

Eric F. Johnson, T. DeWeese, X. Liu, 2007 .

Trifluoromethyl ketones as inhibitors of histone deacetylase.

K. Glaser, S. Davidsen, M. Michaelides, 2002, Bioorganic & medicinal chemistry letters.

Pyrazolo[3,4-d]pyrimidines as potent inhibitors of the insulin-like growth factor receptor (IGF-IR).

S. Davidsen, Eric F. Johnson, J. Wilsbacher, 2007, Bioorganic & medicinal chemistry letters.

Discovery and SAR of orally efficacious tetrahydropyridopyridazinone PARP inhibitors for the treatment of cancer.

P. Ellis, Eric F. Johnson, X. Liu, 2012, Bioorganic & medicinal chemistry.

ABT-888, an Orally Active Poly(ADP-Ribose) Polymerase Inhibitor that Potentiates DNA-Damaging Agents in Preclinical Tumor Models

Eric F. Johnson, T. DeWeese, X. Liu, 2007, Clinical Cancer Research.

Discovery and SAR of 2-(1-propylpiperidin-4-yl)-1H-benzimidazole-4-carboxamide: A potent inhibitor of poly(ADP-ribose) polymerase (PARP) for the treatment of cancer.

Eric F. Johnson, X. Liu, V. Giranda, 2008, Bioorganic & medicinal chemistry.

Synthesis and SAR of novel, potent and orally bioavailable benzimidazole inhibitors of poly(ADP-ribose) polymerase (PARP) with a quaternary methylene-amino substituent.

Eric F. Johnson, X. Liu, V. Giranda, 2008, Bioorganic & medicinal chemistry letters.

Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics.

Z. Tao, P. Kovar, Zehan Chen, 2007, Bioorganic & medicinal chemistry letters.

7-Aminopyrazolo[1,5-a]pyrimidines as potent multitargeted receptor tyrosine kinase inhibitors.

K. Glaser, S. Davidsen, N. Soni, 2008, Journal of medicinal chemistry.

Discovery of the Poly(ADP-ribose) polymerase (PARP) inhibitor 2-[(R)-2-methylpyrrolidin-2-yl]-1H-benzimidazole-4-carboxamide (ABT-888) for the treatment of cancer.

Eric F. Johnson, X. Liu, V. Giranda, 2009, Journal of medicinal chemistry.

3-amino-benzo[d]isoxazoles as novel multitargeted inhibitors of receptor tyrosine kinases.

K. Glaser, S. Davidsen, N. Soni, 2008, Journal of medicinal chemistry.

Lead optimization of methionine aminopeptidase-2 (MetAP2) inhibitors containing sulfonamides of 5,6-disubstituted anthranilic acids.

Gary T. Wang, Chang H. Park, Jieyi Wang, 2007, Bioorganic & medicinal chemistry letters.

Isoquinoline-pyridine-based protein kinase B/Akt antagonists: SAR and in vivo antitumor activity.

V. Stoll, Eric F. Johnson, X. Liu, 2006, Bioorganic & medicinal chemistry letters.

Discovery and SAR of oxindole-pyridine-based protein kinase B/Akt inhibitors for treating cancers.

Eric F. Johnson, X. Liu, V. Giranda, 2006, Bioorganic & medicinal chemistry letters.

Potent and selective inhibitors of Akt kinases slow the progress of tumors in vivo

Yan Shi, V. Stoll, Eric F. Johnson, 2005, Molecular Cancer Therapeutics.

Aryl ketones as novel replacements for the C-terminal amide bond of succinyl hydroxamate MMP inhibitors.

S. Davidsen, D. Albert, J. Summers, 1998, Bioorganic & medicinal chemistry letters.

Abstract A239: Preclinical characterization of ABT-348, a kinase inhibitor targeting the Aurora, VEGFR/PDGFR, and SRC kinase families.

K. Glaser, S. Davidsen, C. Tse, 2011 .

ABT-869, a multitargeted receptor tyrosine kinase inhibitor: inhibition of FLT3 phosphorylation and signaling in acute myeloid leukemia.

Yujia Dai, K. Glaser, S. Davidsen, 2007, Blood.

Noninvasive molecular imaging of apoptosis in vivo using a modified firefly luciferase substrate, Z-DEVD-aminoluciferin

D. Klaubert, S. Ackler, J. Bouska, 2010, Cell Death and Differentiation.

Preclinical activity of ABT-869, a multitargeted receptor tyrosine kinase inhibitor

K. Glaser, S. Davidsen, Eric F. Johnson, 2005, Molecular Cancer Therapeutics.

Tumor suppression by a rationally designed reversible inhibitor of methionine aminopeptidase-2.

Scott A. Erickson, J. Maris, Chang H. Park, 2003, Cancer research.

Phenoxyphenyl sulfone N-formylhydroxylamines (retrohydroxamates) as potent, selective, orally bioavailable matrix metalloproteinase inhibitors.

Yan Guo, Yujia Dai, S. Davidsen, 2002, Journal of medicinal chemistry.

Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors.

A. Vasudevan, Eric F. Johnson, V. Giranda, 2012, Bioorganic & medicinal chemistry letters.

Why optimize cancer drugs for ADMET

G. Sheppard, J. Bouska, 2005 .

Synthesis and evaluation of a new generation of orally efficacious benzimidazole-based poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors as anticancer agents.

P. Ellis, Eric F. Johnson, N. Soni, 2009, Journal of medicinal chemistry.

1,4-Dihydroindeno[1,2-c]pyrazoles as potent checkpoint kinase 1 inhibitors: extended exploration on phenyl ring substitutions and preliminary ADME/PK studies.

Philip J. Merta, Z. Tao, Y. Tong, 2007, Bioorganic & medicinal chemistry letters.

Discovering novel ligands for macromolecules using X-ray crystallographic screening

Vicki L. Nienaber, Paul L. Richardson, Jonathan Greer, 2000, Nature Biotechnology.

Alpha-keto amides as inhibitors of histone deacetylase.

K. Glaser, S. Davidsen, P. Richardson, 2003, Bioorganic & Medicinal Chemistry Letters.

Syntheses of potent, selective, and orally bioavailable indazole-pyridine series of protein kinase B/Akt inhibitors with reduced hypotension.

V. Stoll, G. Gintant, Eric F. Johnson, 2007, Journal of medicinal chemistry.

Glucuronidation of zileuton (A-64077) by human hepatic microsomes.

J. Bouska, D. Sweeny, H. Nellans, 1992, Drug metabolism and disposition: the biological fate of chemicals.

Heterocyclic ketones as inhibitors of histone deacetylase.

K. Glaser, S. Davidsen, A. Vasudevan, 2003, Bioorganic & medicinal chemistry letters.

α-Keto amides as inhibitors of histone deacetylase

Paul L. Richardson, Zhiqin Ji, Jun Guo, 2003 .

Development of multitargeted inhibitors of both the insulin-like growth factor receptor (IGF-IR) and members of the epidermal growth factor family of receptor tyrosine kinases.

Scott A. Erickson, S. Davidsen, Eric F. Johnson, 2009, Bioorganic & medicinal chemistry letters.

Correlation of tumor growth suppression and methionine aminopetidase-2 activity blockade using an orally active inhibitor

Qian Zhang, L. Tucker, Jieyi Wang, 2008, Proceedings of the National Academy of Sciences.

Naphthamidine urokinase plasminogen activator inhibitors with improved pharmacokinetic properties.

Milan Bruncko, V. Giranda, D. Sauer, 2005, Bioorganic & medicinal chemistry letters.

Discovery of the Poly(ADP-ribose) polymerase (PARP) inhibitor 2-[(R)-2-methylpyrrolidin-2-yl]-1H-benzimidazole-4-carboxamide (ABT-888) for the treatment of cancer.

Eric F. Johnson, X. Liu, V. Giranda, 2009, Journal of medicinal chemistry.