List of works - Kent D. Stewart

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

scientific article published on 25 April 2007

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

scientific article published on 17 June 2008

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

scientific article

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

scientific article published in October 2004

An unusual intramolecular hetero-Diels-Alder cycloaddition

scientific article published on 01 April 2005

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

scientific article published on June 15, 2013

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

scientific article

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

scientific article published in August 2003

Cheminformatic tools for medicinal chemists.

scientific article published in July 2010

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

scientific article

Contribution of indazolinone tautomers to kinase activity.

scientific article

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

scientific article published on 01 June 2006

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

scientific article published on 21 August 2007

Design and synthesis of tricyclic cores for kinase inhibition.

scientific article published on 5 December 2012

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

scientific article published in January 2005

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

scientific article

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

scientific article published on 01 November 2006

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

scientific article

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

scientific article published on 01 October 2006

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.

scientific article published on 25 August 2007

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.

scientific article published on 8 March 2007

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

scientific article published on 01 March 1998

Discovery of potent and selective thienopyrimidine inhibitors of Aurora kinases ⬇️

scientific article published on June 29, 2011

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

scientific article

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

scientific article published on 25 July 2006

Establishment and characterization of 7 new monoclonal antibodies to tissue inhibitor of metalloproteinases-1.

scientific article

Hepatitis C NS5B polymerase inhibitors: Functional equivalents for the benzothiadiazine moiety ⬇️

scientific article published on January 13, 2011

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

scientific article

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

scientific article published on 05 June 2006

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

scientific article published on 13 November 2006

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

scientific article

Isoindolinone ureas: a novel class of KDR kinase inhibitors.

scientific article published on September 2004

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

scientific article

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.

scientific article

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

scientific article

Mutations conferring resistance to a potent hepatitis C virus serine protease inhibitor in vitro

scientific article

New shapes in HIV protease inhibitors

scientific article published on 01 October 1990

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

scientific article

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

scientific article

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

scientific article

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

scientific article published on 10 March 2008

Species specificity of amidine-based urokinase inhibitors.

scientific article published in August 2001

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

scientific article published on 8 September 2015

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

scientific article published on 13 March 2007

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

scientific article published on 17 January 2018

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

scientific article

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

scientific article published on 01 May 2002

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

scientific article published on 01 May 1988

Thienopyridine urea inhibitors of KDR kinase.

scientific article published on 9 December 2006

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

scientific article

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

scientific article

Xanthine mimetics as potent dipeptidyl peptidase IV inhibitors.

scientific article published on 28 September 2006

List of works by Kent D. Stewart

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

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

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

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

An unusual intramolecular hetero-Diels-Alder cycloaddition

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

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

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

Cheminformatic tools for medicinal chemists.

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

Contribution of indazolinone tautomers to kinase activity.

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

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

Design and synthesis of tricyclic cores for kinase inhibition.

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

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

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

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

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

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.

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.

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

Discovery of potent and selective thienopyrimidine inhibitors of Aurora kinases ⬇️

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

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

Establishment and characterization of 7 new monoclonal antibodies to tissue inhibitor of metalloproteinases-1.

Hepatitis C NS5B polymerase inhibitors: Functional equivalents for the benzothiadiazine moiety ⬇️

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

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

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

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

Isoindolinone ureas: a novel class of KDR kinase inhibitors.

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

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.

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

Mutations conferring resistance to a potent hepatitis C virus serine protease inhibitor in vitro

New shapes in HIV protease inhibitors

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

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

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

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

Species specificity of amidine-based urokinase inhibitors.

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

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

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

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

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

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

Thienopyridine urea inhibitors of KDR kinase.

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

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

Xanthine mimetics as potent dipeptidyl peptidase IV inhibitors.