K. Stewart

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.

Host-guest complexation. 42. Preorganization strongly enhances the tendancy of hemispherands to form hemispheraplexes

C. Knobler, D. Cram, K. Stewart, 1987 .

Structure of a secreted aspartic protease from C. albicans complexed with a potent inhibitor: Implications for the design of antifungal agents

J. Navaza, C. Abad-Zapatero, S. Muchmore, 1996, Protein science : a publication of the Protein Society.

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.

Conserved residues in the coiled-coil pocket of human immunodeficiency virus type 1 gp41 are essential for viral replication and interhelical interaction.

A. Molla, H. Mo, K. Swift, 2004, Virology.

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 4'-(1,4-dihydro-indeno[1,2-c]pyrazol-3-yl)-benzonitriles and 4'-(1,4-dihydro-indeno[1,2-c]pyrazol-3-yl)-pyridine-2'-carbonitriles as potent checkpoint kinase 1 (Chk1) inhibitors.

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.

The Secreted Proteinases from Candida: Challenges for Structure-Aided Drug Design

C. Abad-Zapatero, K. Stewart, R. Goldman, 1999 .

Synthesis and biological evaluation of 5-substituted 1,4-dihydroindeno[1,2-c]pyrazoles as multitargeted receptor tyrosine kinase inhibitors.

I. Akritopoulou‐Zanze, T. Sowin, D. Albert, 2007, Bioorganic & medicinal chemistry letters.

Formation, isolation and characterization of an AB-biaryl atropisomer of oritavancin

E. Matayoshi, E. Kristensen, K. Stewart, 2004 .

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

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

Aryl uracil inhibitors of hepatitis C virus NS5B polymerase: synthesis and characterization of analogs with a fused 5,6-bicyclic ring motif.

K. Longenecker, A. C. Krueger, A. Molla, 2013, Bioorganic & medicinal chemistry letters.

Hepatitis C NS5B polymerase inhibitors: 4,4-Dialkyl-1-hydroxy-3-oxo-3,4-dihydronaphthalene-3-yl benzothiadiazine derivatives.

V. Stoll, A. Molla, D. Kempf, 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.

Pyrrolidine-constrained phenethylamines: The design of potent, selective, and pharmacologically efficacious dipeptidyl peptidase IV (DPP4) inhibitors from a lead-like screening hit.

G. L. Hamilton, K. Longenecker, H. Sham, 2007, Bioorganic & medicinal chemistry letters.

Survey of the DNA binding properties of natural and synthetic polyamino compounds

K. Stewart, T. A. Gray, T. Gray, 1992 .

The effect of structural changes in a polyamine backbone on its DNA-binding properties.

K. Stewart, 1988, Biochemical and biophysical research communications.

Pharmacological and functional comparison of the polo-like kinase family: insight into inhibitor and substrate specificity.

Eric F. Johnson, V. Giranda, Yan Luo, 2007, Biochemistry.

Xanthine mimetics as potent dipeptidyl peptidase IV inhibitors.

K. Longenecker, H. Sham, K. Stewart, 2006, Bioorganic & medicinal chemistry letters.

In Vitro Selection and Characterization of Influenza A (A/N9) Virus Variants Resistant to a Novel Neuraminidase Inhibitor, A-315675

V. Stoll, A. Molla, D. Kempf, 2002, Journal of Virology.

Species specificity of amidine-based urokinase inhibitors.

P. Richardson, V. Giranda, S. Dorwin, 2001, Biochemistry.

Discovery of 2-[4-{{2-(2S,5R)-2-cyano-5-ethynyl-1-pyrrolidinyl]-2-oxoethyl]amino]- 4-methyl-1-piperidinyl]-4-pyridinecarboxylic acid (ABT-279): a very potent, selective, effective, and well-tolerated inhibitor of dipeptidyl peptidase-IV, useful for the treatment of diabetes.

K. Longenecker, J. Segreti, H. Sham, 2006, Journal of medicinal chemistry.

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.

Isoxazolo[3,4-b]quinoline-3,4(1H,9H)-diones as unique, potent and selective inhibitors for Pim-1 and Pim-2 kinases: chemistry, biological activities, and molecular modeling.

Eric F. Johnson, N. Soni, V. Giranda, 2008, Bioorganic & medicinal chemistry letters.

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

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

Novel transient receptor potential vanilloid 1 receptor antagonists for the treatment of pain: structure-activity relationships for ureas with quinoline, isoquinoline, quinazoline, phthalazine, quinoxaline, and cinnoline moieties.

A. Gomtsyan, Jill M. Wetter, Chih-Hung Lee, 2005, Journal of medicinal chemistry.

Azaindole-Based Inhibitors of Cdc7 Kinase: Impact of the Pre-DFG Residue, Val 195.

K. Swinger, Eric F. Johnson, N. Soni, 2013, ACS medicinal chemistry letters.

Discovery and structure-activity relationships of piperidinone- and piperidine-constrained phenethylamines as novel, potent, and selective dipeptidyl peptidase IV inhibitors.

K. Longenecker, H. Sham, Xiaofen Li, 2007, Journal of medicinal chemistry.

Candida proteases and their inhibition: prospects for antifungal therapy.

C. Abad-Zapatero, K. Stewart, 2001, Current medicinal chemistry.

Structure of Secreted Aspartic Proteinases from Candida

S. Foundling, C. Abad-Zapatero, S. Muchmore, 1998 .

Discovery of a new cyclooxygenase-2 lead compound through 3-D database searching and combinatorial chemistry.

K. Stewart, K. Hulkower, K D Stewart, 1998, Bioorganic & medicinal chemistry letters.

Synthesis of an influenza neuraminidase inhibitor intermediate via a highly diastereoselective coupling reaction.

K. Stewart, D. Barnes, Maureen A. McLaughlin, 2002, Organic letters.

Structure-based design, synthesis, and biological evaluation of potent and selective macrocyclic checkpoint kinase 1 inhibitors.

Chang Park, Philip J. Merta, Z. Tao, 2007, Journal of medicinal chemistry.

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

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

Isoindolinone ureas: a novel class of KDR kinase inhibitors.

K. Glaser, S. Davidsen, M. Michaelides, 2004, Bioorganic & medicinal chemistry letters.

Hepatitis C NS5B polymerase inhibitors: functional equivalents for the benzothiadiazine moiety.

V. Stoll, A. Molla, D. Kempf, 2011, Bioorganic & medicinal chemistry letters.

Synthesis and biological characterization of B-ring amino analogues of potent benzothiadiazine hepatitis C virus polymerase inhibitors.

A. Molla, D. Kempf, J. Randolph, 2009, Journal of medicinal chemistry.

Design and synthesis of tricyclic cores for kinase inhibition.

Brian J. Kotecki, Philip J. Merta, S. Shekhar, 2013, Bioorganic & medicinal chemistry letters.

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

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

Scaffold oriented synthesis. Part 2: Design, synthesis and biological evaluation of pyrimido-diazepines as receptor tyrosine kinase inhibitors.

Zhiqin Ji, Irini Akritopoulou-Zanze, K. Glaser, 2008, Bioorganic & medicinal chemistry letters.

Host-guest complexation. 40. Synthesis and complexation of macrocyclic hosts containing cyclic ureas, anisyls, and steric barriers

C. Knobler, D. Cram, M. Miesch, 1986 .

Complementary solutes enter nonpolar preorganized cavities in lipophilic noncomplementary media

D. Cram, K. Trueblood, I. Goldberg, 1985 .

Influenza neuraminidase inhibitors: structure-based design of a novel inhibitor series.

Jonathan Greer, V. Stoll, J. Greer, 2003, Biochemistry.

Identification of novel binding interactions in the development of potent, selective 2-naphthamidine inhibitors of urokinase. Synthesis, structural analysis, and SAR of N-phenyl amide 6-substitution.

V. Giranda, M. Wendt, V. Nienaber, 2004, Journal of medicinal chemistry.

The 2.2 A structure of the rRNA methyltransferase ErmC' and its complexes with cofactor and cofactor analogs: implications for the reaction mechanism.

C. Abad-Zapatero, G. Schluckebier, K. Stewart, 1999, Journal of molecular biology.

Oral presentations

K. Stewart, B. Willinger, 1999 .

Design, synthesis, and neuraminidase inhibitory activity of GS-4071 analogues that utilize a novel hydrophobic paradigm.

V. Stoll, D. Kempf, W. G. Laver, 2002, Bioorganic & medicinal chemistry letters.

Mutations Conferring Resistance to a Hepatitis C Virus (HCV) RNA-Dependent RNA Polymerase Inhibitor Alone or in Combination with an HCV Serine Protease Inhibitor In Vitro

Kent D. Stewart, Teresa Ng, Rubina Mondal, 2005, Antimicrobial Agents and Chemotherapy.

Lack of stereospecificity in the binding of the P2 amino acid of ritonavir to HIV protease

A. D. Rodrigues, S. Muchmore, A. Molla, 1997 .

Mutations Conferring Resistance to a Potent Hepatitis C Virus Serine Protease Inhibitor In Vitro

A. Molla, H. Mo, T. Pilot‐Matias, 2004, Antimicrobial Agents and Chemotherapy.

Identification and characterization of mutations conferring resistance to an HCV RNA-dependent RNA polymerase inhibitor in vitro.

H. Mo, T. Pilot‐Matias, K. Stewart, 2007, Antiviral research.

Identification and Structural Characterization of I84C and I84A Mutations That Are Associated with High-Level Resistance to Human Immunodeficiency Virus Protease Inhibitors and Impair Viral Replication

A. Molla, D. Kempf, N. Parkin, 2006, Antimicrobial Agents and Chemotherapy.

Characterization of resistant HIV variants generated by in vitro passage with lopinavir/ritonavir.

A. Molla, D. Kempf, H. Mo, 2003, Antiviral research.

Discovery of ((4R,5S)-5-amino-4-(2,4,5- trifluorophenyl)cyclohex-1-enyl)-(3- (trifluoromethyl)-5,6-dihydro- [1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)methanone (ABT-341), a highly potent, selective, orally efficacious, and safe dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.

K. Longenecker, H. Sham, R. Fryer, 2006, Journal of medicinal chemistry.

The D-Alanyl carrier protein in Lactobacillus casei: cloning, sequencing, and expression of dltC

K. Stewart, F. Neuhaus, R. H. Lambalot, 1996, Journal of bacteriology.

Structure-directed discovery of potent non-peptidic inhibitors of human urokinase that access a novel binding subsite.

Jean M. Severin, R A Smith, V. Giranda, 2000, Structure.

Crystal structures of DPP-IV (CD26) from rat kidney exhibit flexible accommodation of peptidase-selective inhibitors.

Vincent S Stoll, K. Longenecker, V. Stoll, 2006, Biochemistry.

Imidazo[2,1-b]thiazoles: multitargeted inhibitors of both the insulin-like growth factor receptor and members of the epidermal growth factor family of receptor tyrosine kinases.

Scott A. Erickson, S. Davidsen, K. Swinger, 2010, Bioorganic & medicinal chemistry letters.

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.

Discovery of 1,4-dihydroindeno[1,2-c]pyrazoles as a novel class of potent and selective checkpoint kinase 1 inhibitors.

Chang Park, Saul H Rosenberg, Y. Tong, 2007, Bioorganic & medicinal chemistry.

Structure of the gene encoding rat thyrotropin releasing hormone.

R. Goodman, K. Stewart, S. L. Lee, 1988, The Journal of biological chemistry.

1,4-Dihydroindeno[1,2-c]pyrazoles as novel multitargeted receptor tyrosine kinase inhibitors.

S. Davidsen, I. Akritopoulou‐Zanze, M. Michaelides, 2006, Bioorganic & Medicinal Chemistry Letters.

Synthesis and activity of N-acyl azacyclic urea HIV-1 protease inhibitors with high potency against multiple drug resistant viral strains.

V. Stoll, S. Vasavanonda, D. Norbeck, 2005, Bioorganic & medicinal chemistry letters.

Hit-to-lead optimization of 1,4-dihydroindeno[1,2-c]pyrazoles as a novel class of KDR kinase inhibitors.

I. Akritopoulou‐Zanze, M. Michaelides, T. Sowin, 2006, Bioorganic & medicinal chemistry letters.

An intramolecular ionic hydrogen bond stabilizes a cis amide bond rotamer of a ring‐opened rapamycin‐degradation product

K. Stewart, M. Dhaon, C. C. Zhou, 2005, Magnetic resonance in chemistry : MRC.

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.

Interaction with the S1 beta-pocket of urokinase: 8-heterocycle substituted and 6,8-disubstituted 2-naphthamidine urokinase inhibitors.

V. Giranda, M. Wendt, V. Nienaber, 2004, Bioorganic & medicinal chemistry letters.

Transforming growth factor beta mimetics: discovery of 7-[4-(4-cyanophenyl)phenoxy]-heptanohydroxamic acid, a biaryl hydroxamate inhibitor of histone deacetylase.

K. Glaser, H. Moses, G. Sheppard, 2002, Molecular cancer therapeutics.

Molecular basis for potentiation of bleomycin‐mediated degradation of DNA by polyamines. Experimental and molecular mechanical studies

L. Strekowski,, W. Wilson, K. Stewart, 1989, Journal of molecular recognition : JMR.

Drug Guru: a computer software program for drug design using medicinal chemistry rules.

K. Stewart, Kent D Stewart, Melisa Shiroda, 2006, Bioorganic & medicinal chemistry.

Structure activity optimization of 6H-pyrrolo[2,3-e][1,2,4]triazolo[4,3-a]pyrazines as Jak1 kinase inhibitors.

Ana L. Aguirre, E. Tarcsa, Bin Li, 2015, Bioorganic & medicinal chemistry letters.

Non-peptide entry inhibitors of HIV-1 that target the gp41 coiled coil pocket.

Kent D. Stewart, Vincent S. Stoll, Jeffrey R. Huth, 2010, Bioorganic & medicinal chemistry letters.

An 'inside-the-box' approach to drug resistance.

D. Kempf, K. Stewart, 2004, Chemistry & biology.

Structure-based characterization and optimization of novel hydrophobic binding interactions in a series of pyrrolidine influenza neuraminidase inhibitors.

Vincent S Stoll, A. C. Krueger, V. Stoll, 2005, Journal of medicinal chemistry.

A novel, picomolar inhibitor of human immunodeficiency virus type 1 protease.

A. Molla, S. Vasavanonda, N. Lyons, 1996, Journal of medicinal chemistry.

Conveyance of partial agonism/antagonism to bombesin/gastrin-releasing peptide analogues on Swiss 3T3 cells by a carboxyl-terminal leucine insertion.

B. Stockstill, J. Leban, K. Stewart, 1992, The Journal of biological chemistry.

Synthesis and Biological Characterization of Aryl Uracil Inhibitors of Hepatitis C Virus NS5B Polymerase: Discovery of ABT-072, a trans-Stilbene Analog with Good Oral Bioavailability.

K. Longenecker, A. C. Krueger, A. Molla, 2018, Journal of medicinal chemistry.

X-ray crystallographic structure of ABT-378 (lopinavir) bound to HIV-1 protease.

V. Stoll, R. Simmer, D. Norbeck, 2002, Bioorganic & medicinal chemistry.

Cheminformatic tools for medicinal chemists.

P. Hajduk, S. Muchmore, K. Stewart, 2010, Journal of medicinal chemistry.

Design, synthesis, and structural analysis of inhibitors of influenza neuraminidase containing a 2,3-disubstituted tetrahydrofuran-5-carboxylic acid core.

V. Stoll, D. Kempf, T. Sowin, 2005, Bioorganic & medicinal chemistry letters.

Design, synthesis, and structural analysis of influenza neuraminidase inhibitors containing pyrrolidine cores.

W G Laver, S. Muchmore, V. Giranda, 2001, Journal of medicinal chemistry.

Discovery, structure-activity relationship, and pharmacological evaluation of (5-substituted-pyrrolidinyl-2-carbonyl)-2-cyanopyrrolidines as potent dipeptidyl peptidase IV inhibitors.

H. Sham, Xiaofen Li, D. Beno, 2006, Journal of Medicinal Chemistry.

Pharmacology and Therapeutic Potential of Benzothiazole Analogues for Cocaine Use Disorder

A. Newman, Alessandro Bonifazi, S. Hemby, 2023, Journal of medicinal chemistry.

Naphthamidine urokinase plasminogen activator inhibitors with improved pharmacokinetic properties.

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

DOCKing ligands into receptors: The test case of α-chymotrypsin

Michael Cory, Kent D. Stewart, James A. Bentley, 1990 .

Design and characterization of an engineered gp41 protein from human immunodeficiency virus-1 as a tool for drug discovery

Kevin Harris, Kent D. Stewart, Kevin Steffy, 2007, J. Comput. Aided Mol. Des..

Catalytic oxidation of dithiols by a semisynthetic enzyme

C. Radziejewski, E. Kaiser, K. Stewart, 1986 .

Contribution of indazolinone tautomers to kinase activity.

A. Vasudevan, C. Abad-Zapatero, K. Stewart, 2012, Bioorganic & medicinal chemistry letters.