J. Stafford

发表

Discovery and evaluation of 2-anilino-5-aryloxazoles as a novel class of VEGFR2 kinase inhibitors.

P. A. Harris, J. Veal, Liping Wang, 2005, Journal of medicinal chemistry.

Discovery of 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methyl-benzenesulfonamide (Pazopanib), a novel and potent vascular endothelial growth factor receptor inhibitor.

P. A. Harris, J. Veal, Rakesh Kumar, 2008, Journal of medicinal chemistry.

Design and synthesis of conformationally constrained analogues of 4-(3-butoxy-4-methoxybenzyl)imidazolidin-2-one (Ro 20-1724) as potent inhibitors of cAMP-specific phosphodiesterase.

J. Veal, F. Schoenen, J. Stafford, 1995, Journal of medicinal chemistry.

Chapter 8. Chronic Pulmonary Inflammation and Other Therapeutic Applications of PDE IV Inhibitors

J. Stafford, P. Feldman, 1996 .

Design and synthesis of pyrimidinone and pyrimidinedione inhibitors of dipeptidyl peptidase IV.

D. Kassel, S. L. Gwaltney, K. Aertgeerts, 2011, Journal of medicinal chemistry.

CNS 7056: A Novel Ultra–short-acting Benzodiazepine

Gavin Kilpatrick, J. Stafford, G. J. Pacofsky, 2007, Anesthesiology.

Design, synthesis and biological evaluation of novel 4-phenylisoquinolinone BET bromodomain inhibitors.

J. Veal, D. Hosfield, Jiangchun Xu, 2018, Bioorganic & medicinal chemistry letters.

Correlation of anti-tumor and anti-angiogenic activity of VEGFR inhibitors with inhibition of VEGFR2 phosphorylation in mice

C. Miller, L. Harrington, T. Gilmer, 2005 .

Antitumour efficacy of VEGFR2 tyrosine kinase inhibitor correlates with expression of VEGF and its receptor VEGFR2 in tumour models

C. Miller, M. Cheung, J. Stafford, 2004, British Journal of Cancer.

Discovery of CC-90011: A Potent and Selective Reversible Inhibitor of Lysine Specific Demethylase 1 (LSD1).

J. Veal, D. Hosfield, L. Lawton, 2020, Journal of medicinal chemistry.

Efficient and regioselective synthesis of 2-alkyl-2H-indazoles.

J. Stafford, Amogh Boloor, M. Cheung, 2003, The Journal of organic chemistry.

Structure-based design and discovery of potent and selective lysine-specific demethylase 1 (LSD1) inhibitors.

J. Veal, Jiangchun Xu, J. D. Del Rosario, 2019, Bioorganic & medicinal chemistry letters.

Kinase Inhibitor Drugs

Rongshi Li, J. Stafford, 2009 .

Overcoming Preclinical Safety Obstacles to Discover (S)-N-((1,2,3,5,6,7-Hexahydro-s-indacen-4-yl)carbamoyl)-6-(methylamino)-6,7-dihydro-5H-pyrazolo[5,1-b][1,3]oxazine-3-sulfonamide (GDC-2394): A Potent and Selective NLRP3 Inhibitor.

Matthew S. Johnson, M. Ultsch, J. Veal, 2022, Journal of medicinal chemistry.

Discovery of TAK-960: an orally available small molecule inhibitor of polo-like kinase 1 (PLK1).

V. Feher, D. Hosfield, T. Kawamoto, 2013, Bioorganic & medicinal chemistry letters.

Daphniphyllum alkaloids. Part 8. Asymmetric total synthesis of (-)-secodaphniphylline

J. Stafford, C. Heathcock, 1990 .

Asymmetric total synthesis of (-)-secodaphniphylline

J. Stafford, C. Heathcock, 1990 .

An efficient and mild synthesis of highly substituted imidazoles

J. Stafford, M. Brackeen, P. Feldman, 1994 .

Relating the structure, activity, and physical properties of ultrashort-acting benzodiazepine receptor agonists.

J. Stafford, G. J. Pacofsky, P. Feldman, 2002, Bioorganic & medicinal chemistry letters.

A highly selective protocol for the deprotection of BOC-protected amides and carbamates

J. Stafford, M. Brackeen, D. Karanewsky, 1993 .

Identification and structure-activity studies of novel ultrashort-acting benzodiazepine receptor agonists.

J. Stafford, G. J. Pacofsky, P. Feldman, 2002, Bioorganic & medicinal chemistry letters.

Efficient and regioselective synthesis of 2-alkyl-2H-indazoles.

J. Stafford, Amogh Boloor, M. Cheung, 2003, The Journal of organic chemistry.

Daphniphyllum alkaloids. 14. Total synthesis of (.+-.)-bukittinggine

J. Stafford, D. L. Clark, C. Heathcock, 1992 .

Degradative Rearrangements of N-(t-Butyloxycarbonyl)-O-methanesulfonyl-hydroxamic Acids: A Novel, Reagent-Based Alternative to the Lossen Rearrangement1

J. Stafford, P. Feldman, Stephen S. Gonzales, 1998 .

An Efficient Method for the Preparation of Alkylidenecyclopropanes.

J. Mcmurry, J. Stafford, 1988 .

An efficient method for the preparation of alkylidenecyclopropanes

J. Mcmurry, J. Stafford, 1988 .

Benzodiazepines a action breve

J. Stafford, G. J. Pacofsky, P. Feldman, 2000 .

Inhibitors of Dipeptidyl Peptidase 4

S. L. Gwaltney, J. Stafford, Jeffrey A. Stafford, 2005 .

KDM4 Inhibition Targets Breast Cancer Stem-like Cells.

Nicola Iovino, M. Boerries, E. Stickeler, 2017, Cancer research.

Structure-based design and SAR development of 5,6-dihydroimidazolo[1,5-f]pteridine derivatives as novel Polo-like kinase-1 inhibitors.

Yan Liu, Jeffrey Stafford, David Hosfield, 2017, Bioorganic & medicinal chemistry letters.

Phosphodiesterase type IV (PDE IV) inhibition. Synthesis and evaluation of a series of 1,3,4-trisubstituted pyrrolidines

J. Stafford, D. Cowan, P. Domanico, 1995 .

Pharmacokinetic-pharmacodynamic correlation from mouse to human with pazopanib, a multikinase angiogenesis inhibitor with potent antitumor and antiangiogenic activity

Ming-Chih Crouthamel, L. Harrington, T. Gilmer, 2007, Molecular Cancer Therapeutics.

Discovery of a novel and potent series of dianilinopyrimidineurea and urea isostere inhibitors of VEGFR2 tyrosine kinase.

J. Veal, Liping Wang, R. Nolte, 2005, Bioorganic & medicinal chemistry letters.

Structure-based design and discovery of potent and selective KDM5 inhibitors.

J. Veal, D. Hosfield, Jiangchun Xu, 2018, Bioorganic & medicinal chemistry letters.

Intramolecular Diels–Alder synthesis of 7-aza-α-carboline compounds

J. Stafford, N. Scorah, Dong Qing, 2010 .

Intramolecular Diels—Alder Synthesis of 7-Aza-α-carboline Compounds.

J. Stafford, N. Scorah, Dong Qing, 2010 .

Design of KDM4 Inhibitors with Antiproliferative Effects in Cancer Models.

J. Veal, T. Bonaldi, D. Hosfield, 2017, ACS medicinal chemistry letters.

Phosphodiesterase type IV inhibition. Structure-activity relationships of 1,3-disubstituted pyrrolidines.

F. Schoenen, J. Stafford, M. A. Leesnitzer, 1995, Journal of medicinal chemistry.

Discovery of alogliptin: a potent, selective, bioavailable, and efficacious inhibitor of dipeptidyl peptidase IV.

D. Kassel, S. L. Gwaltney, K. Takeuchi, 2007, Journal of medicinal chemistry.

TACH101, a first-in-class pan-inhibitor of KDM4 histone demethylase.

J. D. Del Rosario, J. Stafford, E. Filvaroff, 2023, Anti-Cancer Drugs.

Inhibition of VEGF receptors significantly impairs mammary cancer growth in C3(1)/Tag transgenic mice through antiangiogenic and non-antiangiogenic mechanisms

H. Kleinman, Jeffrey E. Green, Rakesh Kumar, 2005, Oncogene.

Inhibition of VEGF receptors significantly impairs mammary cancer growth in C3(1)/Tag transgenic mice through antiangiogenic and non-antiangiogenic mechanisms

H. Kleinman, Jeffrey E. Green, Rakesh Kumar, 2005, Oncogene.

Pharmacology of a Potent and Novel Inhibitor of the NOD-Like Receptor Pyrin Domain-Containing Protein 3 (NLRP3) Inflammasome that Attenuates Development of Nonalcoholic Steatohepatitis and Liver Fibrosis

J. Veal, A. Feldstein, J. Stafford, 2023, The Journal of Pharmacology and Experimental Therapeutics.

Structure-activity relationships involving the catechol subunit of rolipram

F. Schoenen, J. Stafford, P. Domanico, 1994 .

JT002, a small molecule inhibitor of the NLRP3 inflammasome for the treatment of autoinflammatory disorders

E. Gelfand, J. Veal, A. Joetham, 2023, Scientific reports.