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Structures of human plasma β–factor XIIa cocrystallized with potent inhibitors

Blood advances, 2018-03, Vol.2 (5), p.549-558

2018

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Selective Chk1 inhibitors differentially sensitize p53‐deficient cancer cells to cancer therapeutics

International journal of cancer, 2006-12, Vol.119 (12), p.2784-2794

2006

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Discovery of Potent, Selective, Orally Bioavailable Stearoyl-CoA Desaturase 1 Inhibitors

Journal of medicinal chemistry, 2007-06, Vol.50 (13), p.3086-3100

2007

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Potent, Orally Active Heterocycle-Based Combretastatin A-4 Analogues: Synthesis, Structure−Activity Relationship, Pharmacokinetics, and In Vivo Antitumor Activity Evaluation

Journal of medicinal chemistry, 2002-04, Vol.45 (8), p.1697-1711

2002

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Design and synthesis of thiophene dihydroisoquinolines as novel BACE1 inhibitors

Bioorganic & medicinal chemistry letters, 2013-05, Vol.23 (10), p.3075-3080

2013

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Novel cinnoline-based inhibitors of LRRK2 kinase activity

Bioorganic & medicinal chemistry letters, 2013-01, Vol.23 (1), p.71-74

2013

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Discovery and development of antimitotic agents that inhibit tubulin polymerisation for the treatment of cancer

Expert opinion on therapeutic patents, 2002-11, Vol.12 (11), p.1663-1702

2002

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Validation of Diacyl Glycerolacyltransferase I as a Novel Target for the Treatment of Obesity and Dyslipidemia Using a Potent and Selective Small Molecule Inhibitor

Journal of medicinal chemistry, 2008-02, Vol.51 (3), p.380-383

2008

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Discovery of piperidine-aryl urea-based stearoyl-CoA desaturase 1 inhibitors

Bioorganic & medicinal chemistry, 2008-08, Vol.18 (15), p.4298-4302

2008

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Triazolopyridazine LRRK2 kinase inhibitors

Bioorganic & medicinal chemistry letters, 2013-04, Vol.23 (7), p.1967-1973

2013

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Design and synthesis of highly selective, orally active Polo-like kinase-2 (Plk-2) inhibitors

Bioorganic & medicinal chemistry letters, 2013-05, Vol.23 (9), p.2743-2749

2013

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Discovery of 4-alkylamino-7-aryl-3-cyanoquinoline LRRK2 kinase inhibitors

Bioorganic & medicinal chemistry letters, 2013-04, Vol.23 (7), p.1974-1977

2013

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Design of an orally efficacious hydroxyethylamine (HEA) BACE-1 inhibitor in a preclinical animal model

Bioorganic & medicinal chemistry letters, 2010-11, Vol.20 (21), p.6231-6236

2010

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Aminopyridine-Based c-Jun N-Terminal Kinase Inhibitors with Cellular Activity and Minimal Cross-Kinase Activity

Journal of medicinal chemistry, 2006-06, Vol.49 (12), p.3563-3580

2006

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Design and synthesis of hydroxyethylamine (HEA) BACE-1 inhibitors: Prime side chromane-containing inhibitors

Bioorganic & medicinal chemistry letters, 2013-08, Vol.23 (16), p.4674-4679

2013

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Design and synthesis of a novel, orally active, brain penetrant, tri-substituted thiophene based JNK inhibitor

Bioorganic & medicinal chemistry letters, 2011-03, Vol.21 (6), p.1838-1843

2011

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Discovery of Potent, Highly Selective, and Orally Bioavailable Pyridine Carboxamide c-Jun NH2-Terminal Kinase Inhibitors

Journal of medicinal chemistry, 2006-07, Vol.49 (15), p.4455-4458

2006

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Discovery of (R)‑4-Cyclopropyl-7,8-difluoro-5-(4-(trifluoromethyl)phenylsulfonyl)-4,5-dihydro‑1H‑pyrazolo[4,3‑c]quinoline (ELND006) and (R)‑4-Cyclopropyl-8-fluoro-5-(6-(trifluoromethyl)pyridin-3-ylsulfonyl)-4,5-dihydro‑2H‑pyrazolo[4,3‑c]quinoline (ELND007): Metabolically Stable γ‑Secretase Inhibitors that Selectively Inhibit the Production of Amyloid‑β over Notch

Journal of medicinal chemistry, 2013-07, Vol.56 (13), p.5261-5274

2013

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Discovery and Structure−Activity Relationships of Piperidinone- and Piperidine-Constrained Phenethylamines as Novel, Potent, and Selective Dipeptidyl Peptidase IV Inhibitors

Journal of medicinal chemistry, 2007-04, Vol.50 (8), p.1983-1987

2007

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Synthesis and Structure−Activity Relationships of N-{3-[2-(4-Alkoxyphenoxy)thiazol-5-yl]-1- methylprop-2-ynyl}carboxy Derivatives as Selective Acetyl-CoA Carboxylase 2 Inhibitors

Journal of medicinal chemistry, 2006-06, Vol.49 (13), p.3770-3773

2006

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Discovery of a new class of 4-anilinopyrimidines as potent c-Jun N-terminal kinase inhibitors: Synthesis and SAR studies

Bioorganic & medicinal chemistry letters, 2007-02, Vol.17 (3), p.668-672

2007

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Human Chk1 Expression Is Dispensable for Somatic Cell Death and Critical for Sustaining G2 DNA Damage Checkpoint

Molecular cancer therapeutics, 2003-06, Vol.2 (6), p.543-548

2003

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Structures of human plasma β–factor XIIa cocrystallized with potent inhibitors

Selective Chk1 inhibitors differentially sensitize p53‐deficient cancer cells to cancer therapeutics

Discovery of Potent, Selective, Orally Bioavailable Stearoyl-CoA Desaturase 1 Inhibitors

Potent, Orally Active Heterocycle-Based Combretastatin A-4 Analogues: Synthesis, Structure−Activity Relationship, Pharmacokinetics, and In Vivo Antitumor Activity Evaluation

Design and synthesis of thiophene dihydroisoquinolines as novel BACE1 inhibitors

Novel cinnoline-based inhibitors of LRRK2 kinase activity

Discovery and development of antimitotic agents that inhibit tubulin polymerisation for the treatment of cancer

Validation of Diacyl Glycerolacyltransferase I as a Novel Target for the Treatment of Obesity and Dyslipidemia Using a Potent and Selective Small Molecule Inhibitor

Discovery of piperidine-aryl urea-based stearoyl-CoA desaturase 1 inhibitors

Triazolopyridazine LRRK2 kinase inhibitors

Design and synthesis of highly selective, orally active Polo-like kinase-2 (Plk-2) inhibitors

Discovery of 4-alkylamino-7-aryl-3-cyanoquinoline LRRK2 kinase inhibitors

Design of an orally efficacious hydroxyethylamine (HEA) BACE-1 inhibitor in a preclinical animal model

Aminopyridine-Based c-Jun N-Terminal Kinase Inhibitors with Cellular Activity and Minimal Cross-Kinase Activity

Design and synthesis of hydroxyethylamine (HEA) BACE-1 inhibitors: Prime side chromane-containing inhibitors

Design and synthesis of a novel, orally active, brain penetrant, tri-substituted thiophene based JNK inhibitor

Selective and Brain-Permeable Polo-like Kinase-2 (Plk-2) Inhibitors That Reduce [alpha]-Synuclein Phosphorylation in Rat Brain

Discovery of Potent, Highly Selective, and Orally Bioavailable Pyridine Carboxamide c-Jun NH2-Terminal Kinase Inhibitors

Discovery and Structure−Activity Relationships of Piperidinone- and Piperidine-Constrained Phenethylamines as Novel, Potent, and Selective Dipeptidyl Peptidase IV Inhibitors

Selective and Brain-Permeable Polo-like Kinase-2 (Plk-2) Inhibitors That Reduce α-Synuclein Phosphorylation in Rat Brain

Synthesis and Structure−Activity Relationships of N-{3-[2-(4-Alkoxyphenoxy)thiazol-5-yl]-1- methylprop-2-ynyl}carboxy Derivatives as Selective Acetyl-CoA Carboxylase 2 Inhibitors

Discovery of a new class of 4-anilinopyrimidines as potent c-Jun N-terminal kinase inhibitors: Synthesis and SAR studies

Discovery, Structure−Activity Relationship, and Pharmacological Evaluation of (5-Substituted-pyrrolidinyl-2-carbonyl)-2-cyanopyrrolidines as Potent Dipeptidyl Peptidase IV Inhibitors

Human Chk1 Expression Is Dispensable for Somatic Cell Death and Critical for Sustaining G2 DNA Damage Checkpoint

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