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Clinical development of galunisertib (LY2157299 monohydrate), a small molecule inhibitor of transforming growth factor-beta signaling pathway

Drug design, development and therapy, 2015-01, Vol.9 (default), p.4479-4499

2015

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Development of TGF-β signalling inhibitors for cancer therapy

Nature reviews. Drug discovery, 2004-12, Vol.3 (12), p.1011-1022

2004

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Synthesis and activity of new aryl- and heteroaryl-substituted 5,6-dihydro-4H-pyrrolo[1,2-b]pyrazole inhibitors of the transforming growth factor-β type I receptor kinase domain

Bioorganic & medicinal chemistry letters, 2004-07, Vol.14 (13), p.3581-3584

2004

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Synthesis and Activity of New Aryl- and Heteroaryl-Substituted Pyrazole Inhibitors of the Transforming Growth Factor-β Type I Receptor Kinase Domain

Journal of medicinal chemistry, 2003-09, Vol.46 (19), p.3953-3956

2003

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Kinetic Characterization of Novel Pyrazole TGF-β Receptor I Kinase Inhibitors and Their Blockade of the Epithelial−Mesenchymal Transition

Biochemistry (Easton), 2005-02, Vol.44 (7), p.2293-2304

2005

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Optimization of a Dihydropyrrolopyrazole Series of Transforming Growth Factor-β Type I Receptor Kinase Domain Inhibitors: Discovery of an Orally Bioavailable Transforming Growth Factor-β Receptor Type I Inhibitor as Antitumor Agent

Journal of medicinal chemistry, 2008-04, Vol.51 (7), p.2302-2306

2008

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Recent Advances in Diaryl Ether Synthesis

Tetrahedron, 2000-07, Vol.56 (29), p.5045-5065

Scott Sawyer, J.

2000

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Carbocyclic[g]indole Inhibitors of Human Nonpancreatic s-PLA2

Journal of medicinal chemistry, 2005-02, Vol.48 (3), p.893-896

2005

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Selective desilylation of tert-butyldimethylsilyl ethers of phenols using potassium fluoride-alumina and ultrasound

Tetrahedron letters, 1991-12, Vol.32 (49), p.7207-7210

1991

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Pharmacologic actions of the second-generation leukotriene B4 receptor antagonist LY293111: in vitro studies

The Journal of pharmacology and experimental therapeutics, 1999-01, Vol.288 (1), p.286

1999

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Design, synthesis, and pharmacological evaluation of potent xanthone dicarboxylic acid leukotriene B4 receptor antagonists

Journal of medicinal chemistry, , Vol.36 (12), p.1726-1734

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Physical properties and synthetic utility of .alpha.-alkoxyorganolithium species as studied through ligand selectivity in tin-lithium exchange

Journal of the American Chemical Society, 1988-02, Vol.110 (3), p.842-853

1988

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Synthetic and Structure/Activity Studies on Acid-Substituted 2-Arylphenols: Discovery of 2-[2-Propyl-3-[3-[2-ethyl-4-(4-fluorophenyl)-5-hydroxyphenoxy]- propoxy]phenoxy]benzoic Acid, a High-Affinity Leukotriene B4 Receptor Antagonist

Journal of medicinal chemistry, 1995-10, Vol.38 (22), p.4411-4432

1995

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1,2-Dibenzamidobenzene Inhibitors of Human Factor Xa

Journal of medicinal chemistry, 2000-03, Vol.43 (5), p.859-872

2000

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Synthesis of Diaryl Ethers, Diaryl Thioethers, and Diarylamines Mediated by Potassium Fluoride-Alumina and 18-Crown-6: Expansion of Scope and Utility(1)

Journal of organic chemistry, 1998-09, Vol.63 (18), p.6338-6343

1998

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Synthesis of Diaryl Ethers, Diaryl Thioethers, and Diarylamines Mediated by Potassium Fluoride−Alumina and 18-Crown-6: Expansion of Scope and Utility1

Journal of organic chemistry, 1998-09, Vol.63 (18), p.6338-6343

1998

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A concise synthesis of quinazolinone TGF-β RI inhibitor through one-pot three-component Suzuki–Miyaura/etherification and imidate–amide rearrangement reactions

Tetrahedron, 2007-11, Vol.63 (47), p.11763-11770

2007

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Quinoline-substituted dihydroindoles as cysLT1 (LTD4 receptor) antagonists

Bioorganic & medicinal chemistry letters, 1996-02, Vol.6 (3), p.249-252

1996

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Development of TGF-[beta] signalling inhibitors for cancer therapy

Nature reviews. Drug discovery, 2004-12, Vol.3 (12), p.1011

2004

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Biphenylyl-substituted xanthones: highly potent leukotriene B4 receptor antagonists

Journal of medicinal chemistry, , Vol.36 (24), p.3982-3984

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Development of a series of phenyltetrazole leukotriene D4(LTD4) receptor antagonists

Journal of medicinal chemistry, 1992-04, Vol.35 (7), p.1191-1200

1992

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N(2)-Aroylanthranilamide inhibitors of human factor Xa

Journal of medicinal chemistry, 2000-03, Vol.43 (5), p.873-882

2000

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N 2-Aroylanthranilamide Inhibitors of Human Factor Xa

Journal of medicinal chemistry, 2000-03, Vol.43 (5), p.873-882

2000

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Carbocyclic[ g ]indole Inhibitors of Human Nonpancreatic s-PLA 2

Journal of medicinal chemistry, 2005-02, Vol.48 (3), p.893-896

2005

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Clinical development of galunisertib (LY2157299 monohydrate), a small molecule inhibitor of transforming growth factor-beta signaling pathway

Development of TGF-β signalling inhibitors for cancer therapy

Synthesis and activity of new aryl- and heteroaryl-substituted 5,6-dihydro-4H-pyrrolo[1,2-b]pyrazole inhibitors of the transforming growth factor-β type I receptor kinase domain

Preclinical assessment of galunisertib (LY2157299 monohydrate), a first-in-class transforming growth factor-β receptor type I inhibitor

Synthesis and Activity of New Aryl- and Heteroaryl-Substituted Pyrazole Inhibitors of the Transforming Growth Factor-β Type I Receptor Kinase Domain

Kinetic Characterization of Novel Pyrazole TGF-β Receptor I Kinase Inhibitors and Their Blockade of the Epithelial−Mesenchymal Transition

Optimization of a Dihydropyrrolopyrazole Series of Transforming Growth Factor-β Type I Receptor Kinase Domain Inhibitors: Discovery of an Orally Bioavailable Transforming Growth Factor-β Receptor Type I Inhibitor as Antitumor Agent

Recent Advances in Diaryl Ether Synthesis

Carbocyclic[g]indole Inhibitors of Human Nonpancreatic s-PLA2

Selective desilylation of tert-butyldimethylsilyl ethers of phenols using potassium fluoride-alumina and ultrasound

Pharmacologic actions of the second-generation leukotriene B4 receptor antagonist LY293111: in vitro studies

Design, synthesis, and pharmacological evaluation of potent xanthone dicarboxylic acid leukotriene B4 receptor antagonists

Physical properties and synthetic utility of .alpha.-alkoxyorganolithium species as studied through ligand selectivity in tin-lithium exchange

Synthetic and Structure/Activity Studies on Acid-Substituted 2-Arylphenols: Discovery of 2-[2-Propyl-3-[3-[2-ethyl-4-(4-fluorophenyl)-5-hydroxyphenoxy]- propoxy]phenoxy]benzoic Acid, a High-Affinity Leukotriene B4 Receptor Antagonist

1,2-Dibenzamidobenzene Inhibitors of Human Factor Xa

Synthesis of Diaryl Ethers, Diaryl Thioethers, and Diarylamines Mediated by Potassium Fluoride-Alumina and 18-Crown-6: Expansion of Scope and Utility(1)

Synthesis of Diaryl Ethers, Diaryl Thioethers, and Diarylamines Mediated by Potassium Fluoride−Alumina and 18-Crown-6: Expansion of Scope and Utility1

A concise synthesis of quinazolinone TGF-β RI inhibitor through one-pot three-component Suzuki–Miyaura/etherification and imidate–amide rearrangement reactions

Quinoline-substituted dihydroindoles as cysLT1 (LTD4 receptor) antagonists

Development of TGF-[beta] signalling inhibitors for cancer therapy

Biphenylyl-substituted xanthones: highly potent leukotriene B4 receptor antagonists

Development of a series of phenyltetrazole leukotriene D4(LTD4) receptor antagonists

N(2)-Aroylanthranilamide inhibitors of human factor Xa

N 2-Aroylanthranilamide Inhibitors of Human Factor Xa

Carbocyclic[ g ]indole Inhibitors of Human Nonpancreatic s-PLA 2

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